Novel 1,3,4-Triaryl Pyrazoles: Synthesis, QSAR Studies and Cytotoxicity against Breast Cancer.

Abstract:

BACKGROUND:The existence of drug-resistance and lack of selectivity encourages scientists to search for novel and more selective cytotoxic agents. OBJECTIVES:In this work, novel 1,3,4-triarylpyrazole derivatives were synthesized to study their cytotoxicity on MCF7 (human breast Cell Line). In addition, QSAR studies were performed to show the relation between the cytotoxic activity and the structural features of our new synthesized pyrazole derivatives. METHODS:Pyrazole-4-carbaldehyde derivative 3 was utilized as a starting material for the preparation of the new pyarazole derivatives. These target compounds were screened for their cytotoxic activity against MCF-7 followed by study cell cycle of the most active compounds. Finally, pharmacophore modeling and QSAR Studies was carried out. RESULTS:Among these compounds; 5d and 8b showed the highest anti-proliferative activity (IC50 = 4.9 and 2.11 µM, respectively). Flow cytometric analysis showed that, compounds 5d and 8b arrested the cell cycle in addition to induction of apoptosis in MCF7 cells. Moreover, their stimulation effect on caspases 3/7 was examined to explore their mechanism of induction of apoptosis and the results showed that their proapoptotic activity could be due to the activation of caspases 3/7. CONCLUSION:Pyrazole derivatives 5d and 8b displayed potent bioactivities, indicating that these compounds could be considered as a new lead for more investigation in the future.

authors

Ismail MMF,Farrag AM,Harras MF

doi

10.2174/1871520619666190207094610

subject

Has Abstract

pub_date

2019-01-01 00:00:00

pages

948-959

issue

7

eissn

1871-5206

issn

1875-5992

pii

ACAMC-EPUB-96472

journal_volume

19

pub_type

杂志文章
  • Conventional chemotherapy and emerging targeted therapy for advanced adrenocortical carcinoma.

    abstract::Adrenocortical carcinoma (ACC) is a rare but typically aggressive malignancy. Radical surgery remains the potentially curative option. However, about one third of patients initially present with distant metastases. Regarding to chemotherapy, mitotane alone or in combination with cytotoxic drugs should be the first sel...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520611313020010

    authors: Xu YZ,Zhu Y

    更新日期:2013-02-01 00:00:00

  • Alkylamino Phenol Derivative Induces Apoptosis by Inhibiting EGFR Signaling Pathway in Breast Cancer Cells.

    abstract:BACKGROUND AND OBJECTIVE:The present study was carried out to evaluate the anticancer property of an alkylamino phenol derivative -2-((3,4-Dihydroquinolin-1(2H)-yl)(p-tolyl)methyl)phenol) (THTMP) against human breast cancer cells. The cytotoxicity of the THTMP was assessed to know its specificity towards breast cancer ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200213101407

    authors: Palanivel S,Yli-Harja O,Kandhavelu M

    更新日期:2020-01-01 00:00:00

  • The Role of Vitamin D and Sunlight Incidence in Cancer.

    abstract:BACKGROUND:Vitamin D (VD) deficiency affects individuals of different ages in many countries. VD deficiency may be related to several diseases, including cancer. OBJECTIVE:This study aimed to review the relationship between VD deficiency and cancer. METHODS:We describe the proteins involved in cancer pathogenesis and...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1389557519666190312123212

    authors: Camara AB,Brandao IA

    更新日期:2019-01-01 00:00:00

  • Combination of DC Vaccine and Conventional Chemotherapeutics.

    abstract::Recently mutual interactions of chemotherapy and immunotherapy have been widely accepted, and several synergistic mechanisms have been elucidated as well. Although much attention has focused on the combination of DC vaccine and chemotherapy, there are still many problems remaining to be resolved, including the optimal...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520615666150907094139

    authors: Dong W,Wei R,Shen H,Ni Y,Meng L,Du J

    更新日期:2016-01-01 00:00:00

  • HCC Specific Protein Network Involving Interactions of EGFR with A-Raf and Transthyretin: Experimental Analysis and Computational Biology Correlates.

    abstract:BACKGROUND:The network interactions link human disease proteins to regulatory cellular pathways leading to better understanding of protein functions and cellular processes. Revealing the network of signaling pathways in cancer through protein-protein interactions at molecular level enhances our understanding of Hepatoc...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520618666180507141632

    authors: Ranjpour M,Katare DP,Wajid S,Jain SK

    更新日期:2018-01-01 00:00:00

  • Ethanolic Extract of Algerian Propolis and Galangin Decreased Murine Melanoma Tumor Progression in Mice

    abstract::Melanoma is the more dangerous skin cancer, and metastatic melanoma still carries poor prognosis. Despite recent therapeutic advances, prolonged survival remains rare and research is still required. Propolis extracts from many countries have attracted a great deal of attention for their biological properties. We here ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520616666160211124459

    authors: Benguedouar L,Lahouel M,Gangloff SC,Durlach A,Grange F,Bernard P,Antonicelli F

    更新日期:2016-01-01 00:00:00

  • Novel molecular anti-colorectalcancer conjugate:chlorambucil-adipic acid dihydrizide-glutamine.

    abstract::Cancer is one of the most fatal diseases in the world and it has been years that finding new drugs and chemotherapeutic techniques with lowest side effects become one of the most important challenging matters needs really hard efforts. Chlorambucil (CBL), an ancient direct-acting alkylating anticancer agent, is common...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/18715206113139990132

    authors: Tabasi MA,Amanlou M,Siadat SD,Nourmohammadi Z,Omoomi FD,Ebrahimi SE,Aghasadeghi MR,Rahimi P,Pourhosseini S,Mehravi B,Ardestani MS

    更新日期:2013-11-01 00:00:00

  • The Antitumor Activity of a Novel Fluorobenzamidine against Dimethylhydrazine- Induced Colorectal Cancer in Rats.

    abstract:BACKGROUND:Colorectal cancer is among the leading causes of death worldwide. The incidence of deaths is expected to be 11.4 million in 2030. OBJECTIVE:We aimed to evaluate the in vitro and in vivo antioxidant and antitumor activities of a novel Bithiophene- Fluorobenzamidine (BFB) against DMH-induced colorectal cancer...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520619666191021162411

    authors: Abdel-Rasol M,El-Beih NM,Yahya SMM,Ismail MA,El-Sayed WM

    更新日期:2020-01-01 00:00:00

  • Dinuclear berenil-platinum (II) complexes as modulators of apoptosis in human MCF-7 and MDA-MB231 breast cancer cells.

    abstract::The metabolism of alkylating agents is accompanied by the generation of reactive oxygen species. The aim of this study was to treat estrogen receptor-positive and estrogen receptor-negative human breast cancer cells, MCF-7 and MDA-MB-231, respectively, with cisplatin and five different berenil-platinum (II) complexes,...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520614666140623120809

    authors: Agnieszka G,Ewa A,Anna B,Krzysztof B,Monika C,Elżbieta S

    更新日期:2014-01-01 00:00:00

  • Lemon Juice as a Biocatalyst Under Ultrasound Irradiation: Synthesis and Pharmacological Evaluation of 2-amino 1,3,4-thiadiazoles.

    abstract:BACKGROUND:The 2-amino 1,3,4-thiadiazole framework has attracted considerable interest because of its prevalence in compounds possessing a wide range of pharmacological properties including anticancer/antitumor activities. Though a number of methods have been reported for the synthesis of this class of compounds, some ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200409143513

    authors: Prasad MG,Lakshmi CV,Katari NK,Pal M

    更新日期:2020-01-01 00:00:00

  • Treatment approaches in elderly patients with head and neck cancer.

    abstract::Integration of geriatric assessment into cancer clinical practice is strongly needed in squamous cell carcinoma of the head and neck (SCCHN) due to the frequent discrepancy between chronologic and biologic age. Comprehensive Geriatric Assessment (CGA) is a multidimensional assessment tool that examines age-related dom...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/18715206113136660355

    authors: Perri F,Ionna F,Pavone E,Longo F,Caponigro F

    更新日期:2013-11-01 00:00:00

  • Effectiveness of two novel anionic and cationic platinum complexes in the treatment of osteosarcoma.

    abstract:AIM:This study aimed to characterize the cellular basis of the platinum cytotoxicity of two novel platinum complexes, 3Pt and 1Pt, in comparison with that of cisplatin. 3Pt comprises anionic phosphate moieties, while 1Pt comprises neutral aromatic ligands. METHODS:We compared the cytotoxic potency of 3Pt and 1Pt with ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520615666141216151547

    authors: Igarashi K,Yamamoto N,Hayashi K,Takeuchi A,Miwa S,Odani A,Tsuchiya H

    更新日期:2015-01-01 00:00:00

  • Withdrawal Notice: Growth Kinetics and Oncologic Outcomes for Small Renal Masses Managed with Active Surveillance: A Review of the Literature

    abstract::The article has been withdrawn at the request of the editor of the journal Anti-Cancer Agents in Medicinal Chemistry. Bentham Science apologizes to the readers of the journal for any inconvenience this may cause. Bentham Science Disclaimer:It is a condition of publication that manuscripts submitted to this journal ha...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520617666171114111053

    authors: Ristau BT,Fuller TW,Rios R,Ho C,Tomaszewski JJ

    更新日期:2017-11-13 00:00:00

  • Synthesis and biological evaluation of novel antifolate analogs as potential anticancer treatment.

    abstract::A novel process for the preparation of two ketomethylenic antifolates, 2-(2-{4-[(2,4-diamino-pteridin-6-ylmethyl)-amino]- phenyl}-2-oxo-ethyl) pentanedioic acid and 2-(2-{4-[(2,4-diamino-pteridin-6-ylmethyl)-methyl-amino]-phenyl}-2-oxo-ethyl) pentanedioic acid is described herein. Both compounds were compared with met...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520611313020022

    authors: Stoicescu DF,Rotaru M

    更新日期:2013-02-01 00:00:00

  • Radiolabelled regulatory peptides for imaging and therapy.

    abstract::Radiolabelled peptides have shown to be an important class of radiopharmaceuticals for imaging and therapy of malignancies expressing receptors of regulatory peptides. These peptides have high affinity and specificity for their receptors. The majority of these receptors are present at different levels in different tis...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152007780618171

    authors: Breeman WA,Kwekkeboom DJ,de Blois E,de Jong M,Visser TJ,Krenning EP

    更新日期:2007-05-01 00:00:00

  • Nicotine, lung and cancer.

    abstract::The respiratory epithelium expresses the cholinergic system including nicotinic receptors (nAChRs). It was reported that normal human bronchial epithelial cells (BEC), which are the precursor for squamous cell carcinomas, and small airway epithelial cells (SAEC), which are the precursor for adenocarcinomas, have sligh...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152007781058587

    authors: Grozio A,Catassi A,Cavalieri Z,Paleari L,Cesario A,Russo P

    更新日期:2007-07-01 00:00:00

  • Effect of selenium-saturated bovine lactoferrin (Se-bLF) on antioxidant enzyme activities in human gut epithelial cells under oxidative stress.

    abstract::Cancer and many chronic inflammatory diseases are associated with increased amounts of reactive oxygen species (ROS). The potential cellular and tissue damage created by ROS has significant impact on many disease and cancer states and natural therapeutics are becoming essential in regulating altered redox states. We h...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/187152011797378616

    authors: Burrow H,Kanwar RK,Mahidhara G,Kanwar JR

    更新日期:2011-10-01 00:00:00

  • Y-shaped Folic Acid-Conjugated PEG-PCL Copolymeric Micelles for Delivery of Curcumin.

    abstract:BACKGROUND:Curcumin is a natural hydrophobic product showing anticancer activity. Many studies show its potential use in the field of cancer treatment due to its safety and efficiency. However, its application is limited due to its low water-solubility and poor selective delivery to cancer. OBJECTIVE:A Y-shaped folic ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520616666160815124014

    authors: Feng R,Zhu W,Chu W,Teng F,Meng N,Deng P,Song Z

    更新日期:2017-01-01 00:00:00

  • Current and emerging strategies in bladder cancer.

    abstract::Urothelial cell carcinoma is one of the most common malignancies of the urinary tract. The standard of care, intravesical chemo- and immunotherapy, while effective, is associated with a considerable side-effect profile and approximately 30% of patients either fail to respond to treatment or suffer recurrent disease wi...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152012800617768

    authors: Carradori S,Cristini C,Secci D,Gulia C,Gentile V,Di Pierro GB

    更新日期:2012-07-01 00:00:00

  • Cilengitide: the first anti-angiogenic small molecule drug candidate design, synthesis and clinical evaluation.

    abstract::Cilengitide, a cyclic RGD pentapeptide, is currently in clinical phase III for treatment of glioblastomas and in phase II for several other tumors. This drug is the first anti-angiogenic small molecule targeting the integrins αvβ3, αvβ5 and αvβ1. It was developed by us in the early 90s by a novel procedure, the spatia...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152010794728639

    authors: Mas-Moruno C,Rechenmacher F,Kessler H

    更新日期:2010-12-01 00:00:00

  • Novel molecular-targeted therapeutics for the treatment of cancer.

    abstract::Recently, intensive laboratory and preclinical studies have identified and validated therapeutic molecular targets in cancer, particularly the receptor tyrosine kinases, the intracellular pathways, and the genetic and epigenetic alterations, resulting in an unprecedented surge of novel, targeted therapies and therapeu...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152008784533099

    authors: Yasui H,Imai K

    更新日期:2008-06-01 00:00:00

  • Deoxypodophyllotoxin isolated from Juniperus communis induces apoptosis in breast cancer cells.

    abstract::The study of anticancer properties from natural products has regained popularity as natural molecules provide a high diversity of chemical structures with specific biological and medicinal activity. Based on a documented library of the most common medicinal plants used by the indigenous people of North America, we scr...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520614666140608150448

    authors: Benzina S,Harquail J,Jean S,Beauregard AP,Colquhoun CD,Carroll M,Bos A,Gray CA,Robichaud GA

    更新日期:2015-01-01 00:00:00

  • Design and Synthesis of Tetrahydroisoquinoline Derivatives as AntiAngiogenesis and Anti-Cancer Agents.

    abstract:AIM:The aim of our research work is the synthesis of tetrahydroisoquinoline derivatives as anti-Angiogenesis and anti-cancer agents. BACKGROUND:Cancer is the second leading cause of deaths in United States. The current recovery rate from the advanced treatment for the cancer is unacceptably low. Therefore, identificat...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520621666210112122913

    authors: Gangapuram M,Eyunni S,Zhang W,Redda KK

    更新日期:2021-01-12 00:00:00

  • Antileukemic Properties of Sesquiterpene Lactones: A Systematic Review.

    abstract::This review summarizes the reported molecular mechanisms underlying the antileukemic property of Sesquiterpene Lactones (SLs). This systematic review was registered in the PROSPERO database and conducted following the PRISMA Statements. The MeSH terms, Sesquiterpenes, Lactones and Leukemia were used in four databases ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520617666170918130126

    authors: da Silva Castro E,Alves Antunes LA,Revoredo Lobo JF,Ratcliffe NA,Borges RM,Rocha L,Burth P,Fonte Amorim LM

    更新日期:2018-01-01 00:00:00

  • Oncologists' current opinion on the treatment of colon carcinoma.

    abstract::Colorectal cancer is a major global health problem with more than a million new cases diagnosed worldwide in 2005. In the United States, this malignancy is the third most common with 145,000 new cases and the second most lethal with 56,000 deaths in 2005. Unfortunately, preclinical diagnostic screening in the U.S. pop...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152007781668742

    authors: Majer M,Akerley W,Kuwada SK

    更新日期:2007-09-01 00:00:00

  • In Vitro Anticancer Effects of Two New Potent Hydrazide Compounds on Leukemic Cells.

    abstract:BACKGROUND:Chronic myeloid leukemia (CML), also recognized as chronic myelogenous leukemia, is initiated in some types of blood-forming cells of the bone marrow. The therapeutic approach to CML is usually chemotherapy; however, severe side effects and complications are major problems in the clinical research. Thus, rec...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520616666160404112945

    authors: Tavakolfar S,Mousavi E,Almasirad A,Amanzadeh A,Atyabi SM,Yaghamii P,Samiee-Sadr S,Salimi M

    更新日期:2016-01-01 00:00:00

  • Killing Glioma 'Stem-like' Cells via Drug-Induced Relocation of Endosomal Urokinase Proteins.

    abstract::High grade gliomas (HGGs) are primary CNS cancers with more than 95% of patients experiencing tumor recurrence following radiation therapy, chemotherapy, and/or an anti-angiogenic therapy. Populations of glioma 'stem-like' cells (GSCs) exist in both proliferative and non-proliferative states and are capable of tumor r...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:

    authors: Gorin FA,Pasupuleti N,Mahajan D,Dugar S

    更新日期:2017-01-01 00:00:00

  • Therapeutic targeting of malignant glioma.

    abstract::Glioblastoma Multiforme (GMB) is the most aggressive primary brain tumor with poor survival rates and universal recurrence despite aggressive treatments. Recent research suggested that GBM has multiple glioma cell populations, some of which are organized in a stem cell hierarchical order with different stages of diffe...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520614666140825105145

    authors: Alexandru-Abrams D,Jadus MR,Hsu FP,Stathopoulos A,Bota DA

    更新日期:2014-01-01 00:00:00

  • lncRNAs as Potential Targets in Small Cell Lung Cancer: MYC -dependent Regulation.

    abstract:BACKGROUND:Small Cell Lung Cancer (SCLC) is a highly aggressive malignancy. MYC family oncogenes are amplified and overexpressed in 20% of SCLCs, showing that MYC oncogenes and MYC regulated genes are strong candidates as therapeutic targets for SCLC. c-MYC plays a fundamental role in cancer stem cell properties and ma...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200721130700

    authors: Tokgun O,Tokgun PE,Inci K,Akca H

    更新日期:2020-01-01 00:00:00

  • Double Edge Sword Behavior of Carbendazim: A Potent Fungicide With Anticancer Therapeutic Properties.

    abstract:BACKGROUND:A number of benzimidazole derivatives such as benomyl and carbendazim have been known for their potential role as agricultural fungicides. Simultaneously carbendazim has also been found to inhibit proliferation of mammalian tumor cells specifically drug and multidrug resistant cell lines. OBJECTIVE:To under...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520616666161221113623

    authors: Goyal K,Sharma A,Arya R,Sharma R,Gupta GK,Sharma AK

    更新日期:2018-01-01 00:00:00