Abstract：
:Benzodiazepines (BZDs) represent a diverse class of bicyclic heterocyclic molecules. In the last few years, benzodiazepines have emerged as potential therapeutic agents. As a result, several mild, efficient and high yielding protocols have been developed that offer access to various functionalized benzodiazepines (BZDs). They are known to possess a wide array of biological activities such as anxiolytic, anticancer, anticonvulsant, antipsychotics, muscle relaxant, anti-tuberculosis, and antimicrobial activities. The fascinating spectrum of biological activities exhibited by BZDs in various fields has prompted the medicinal chemist to design and discover novel benzodiazepine-based analogs as potential therapeutic candidates with the desired biological profile. In this review, an attempt has been made by to summarize (1) Recent advances in the synthetic chemistry of benzodiazepines which enable their synthesis with desired substitution pattern; (2) Medicinal chemistry of BZDs as therapeutic candidates with promising biological profile including insight of mechanistic studies; (3) The correlation of biological data with the structure i.e. structure-activity relationship studies were also included to provide an insight into the rational design of more active agents.
journal_name
Bioorg Chemjournal_title
Bioorganic chemistryauthors
Arora N,Dhiman P,Kumar S,Singh G,Monga Vdoi
10.1016/j.bioorg.2020.103668subject
Has Abstractpub_date
2020-04-01 00:00:00pages
103668eissn
0045-2068issn
1090-2120pii
S0045-2068(19)31074-0journal_volume
97pub_type
杂志文章,评审abstract：:There is much interest in the use of phytoestrogens such as coumestrol in breast cancer intervention due to their antiestrogenic activity and multiple modes of tumor cell death. However, the clear beneficial effects of naturally occurring estrogen mimetic coumestrol remain controversial due to experimental evidence th...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.12.024
更新日期：2019-04-01 00:00:00
abstract：:5-Aryl-1H-tetrazoles (1-24) were synthesized and screened for their xanthine oxidase (XO) inhibitory activity using allopurinol as standard inhibitor (IC50 = 2.0 ± 0.01 µM). Six compounds 3, 4, 5, 9, 21, and 24 exhibited significant to weak activities with IC50 values in the range of 7.4-174.2 µM. Active compounds wer...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.04.021
更新日期：2018-09-01 00:00:00
abstract：:In continuation of our previous work on the investigation of CDK9 inhibitors bearing indole moiety for the discovery of novel anticancer agents, novel methylenehydrazine-1-carboxamide derivatives with (5-((4-(pyridin-3-yl)pyrimidin-2-yl)amino)-1H-indole scaffold were designed, synthesized, and evaluated for the CDK9 i...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104064
更新日期：2020-09-01 00:00:00
abstract：:The design and synthesis of a series of thirty-two halogenated 1-tetralone or 6-amino-1-tetralone chalcone derivatives was achieved by the Claisen-Schmidt condensation reaction and were evaluated for their inhibitory effects against ROS production in LPS-stimulated RAW 264.7 macrophages. It was observed that the intro...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.03.055
更新日期：2019-06-01 00:00:00
abstract：:Combining two bioactive moieties by covalent bond into a novel single hybrid biological entity in view of the principle of active splicing, twenty-two C28-modified derivatives of pentacyclic dihydroxytriterpene carboxylic acids with saturated nitrogen heterocycle segments (i.e. 1-deoxynojirimycin or piperazines) have ...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.103694
更新日期：2020-04-01 00:00:00
abstract：:Novel derivatives of flurbiprofen 1-18 including flurbiprofen hydrazide 1, substituted aroyl hydrazides 2-9, 2-mercapto oxadiazole derivative 10, phenacyl substituted 2-mercapto oxadiazole derivatives 11-15, and benzyl substituted 2-mercapto oxadiazole derivatives 16-18 were synthesized and characterized by EI-MS, 1H ...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.07.038
更新日期：2018-12-01 00:00:00
abstract：:Seven new diterpenoids (1-7), including five 7-membered ring vibsane-type diterpenoids, vibsanolide A-E (1-5) and a pair of epimers of 14,15,16,17-tetranorvibsane-type diterpenoids possessing bicyclo[4.2.1]nonane moiety, vibsanolide F-G (6-7), together with twelve known analogues (8-19) were isolated from the crude ex...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104498
更新日期：2021-01-01 00:00:00
abstract：:Glycyrrhetinic acid has been usually studied for their anti-tumor activities. However, the low bioavailability and poor aqueous solubility as well as limited intracellular accumulation have limited their utility. In this present study, a series of new glycyrrhetinic acid conjugates with a triphenylphosphonium cation (...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.12.036
更新日期：2019-04-01 00:00:00
abstract：:Occurrence of infections due to the drug resistant Staphylococcus aureus is on rise necessitating the need for rapid development of new antibacterial agents. In our present work, a series of new 3-phenylquinazolin-4(3H)-one derivatives were designed, synthesized and evaluated for their antibacterial activity against E...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.08.012
更新日期：2018-12-01 00:00:00
abstract：:Euphoroids A-C (1-3), three new ent-abietane-type diterpenoids, together with ten known analogues (4-13) were obtained from the roots of Euphorbia ebracteolata. The structures of these compounds were determined by extensive spectroscopic data analysis, including UV, HRESIMS, 1D-, and 2D-NMR data. The inhibitory effect...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.07.032
更新日期：2018-12-01 00:00:00
abstract：:The structurally related tetrapyrrolic pigments are a group of natural products that participate in many of the fundamental biosynthetic and catabolic processes of living organisms. Porphobilinogen synthase catalyzes a rate-limiting step for the biosyntheses of tetrapyrrolic natural products. In the present study, a v...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2008.11.001
更新日期：2009-02-01 00:00:00
abstract：:Antiviral alpha-P-borano substituted NTPs are promising chain terminators targeting HIV reverse transcriptase (RT). Activation of antiviral nucleoside diphosphates (NDPs) to NTPs may be carried out by pyruvate kinase (PK) and creatine kinase (CK). Herein, are presented the effects of nucleobase, ribose, and alpha-phos...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2008.03.001
更新日期：2008-08-01 00:00:00
abstract：:Current study is based on the sequential conversion of indolyl butanoic acid (1) into ethyl indolyl butanoate (2), indolyl butanohydrazide (3), and 1,3,4-oxadiazole-2-thiol analogs (4) by adopting chemical transformations. In a parallel series of reactions, 2-bromo-N-phenyl/arylacetamides (7a-l) were synthesized by re...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.08.010
更新日期：2018-12-01 00:00:00
abstract：:A concise chemoenzymatic route toward enantiomerically enriched active pharmaceutical ingredients (API) - diprophylline and xanthinol nicotinate - is reported for the first time. The decisive step is an enantioselective lipase-mediated methanolysis of racemic chlorohydrin-synthon acetate, namely 1-chloro-3-(1,3-dimeth...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104448
更新日期：2021-01-01 00:00:00
abstract：:2-Epi-jaspine B is an isomer of the natural product jaspine B and shows certain selectivity for SphK1 and potent antitumor activity. Based on the crystal structure of SphK1, we transformed the structure of 2-epi-jaspine B and modified the hydrophobic side chain to obtain a series of 2-epi-jaspine B analogs. The MTT as...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103369
更新日期：2020-05-01 00:00:00
abstract：:Building on the conclusions of previous inhibition studies with pyridinium-benzenesulfonamides from our team and on the X-ray crystal structure of the lead compound identified, a series of 24 pyridinium derivatives of 3-aminobenzenesulfonamide was synthesized and investigated for carbonic anhydrase inhibition. The new...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104204
更新日期：2020-10-01 00:00:00
abstract：:Chondrocyte based therapy is promising to treat symptomatic chondral and osteochondral lesions. Growth factors to accelerate the proliferation and retain the phenotype of chondrocytes in vitro are imperative. However, the high cost and rapid degradation of growth factors limited their further application. Therefore, i...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2014.09.005
更新日期：2014-12-01 00:00:00
abstract：:Mitomycin C (MC), an anti-cancer drug, and its analog, decarbamoylmitomycin C (DMC), are DNA-alkylating agents. MC is currently used in the clinics and its cytotoxicity is mainly due to its ability to form Interstrand Crosslinks (ICLs) which impede DNA replication and, thereby, block cancer cells proliferation. Howeve...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103280
更新日期：2019-11-01 00:00:00
abstract：:In addition to its catalytic domain, phosphoinsositide-dependent protein kinase-1 (PDK1) contains a C-terminal pleckstrin homology (PH) domain, which binds the membrane-bound phosphatidylinositol (3,4,5)-triphosphate [PI(3,4,5)P3] second messenger. Here, we report in vitro kinetic, phosphopeptide mapping, and oligomer...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2006.05.002
更新日期：2006-08-01 00:00:00
abstract：:One of the many methods of treating cancer is to terminate the uncontrolled growth of cancer cells. So, aiming the apoptotic pathway is an exciting approach to finding new anticancer agents. A novel series of cyanopyridines was designed and synthesized for antiproliferative evaluation. 2-Amino-6-(4-(benzyloxy)phenyl)-...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103481
更新日期：2020-01-01 00:00:00
abstract：:A series of six novel and six known thieno[2,3-d]pyrimidin-4-amines 2-13 were synthesized, and further were used as a starting material for preparation of a small series of eight novel thieno[2,3-d]pyrimidin-4-phthalimides 14-21. Eight compounds, five amine and three phthalimide derivatives, inhibited bovine pancreati...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2018.07.009
更新日期：2018-10-01 00:00:00
abstract：:P-glycoprotein (P-gp) is one of the cell membrane pumps which mediate the efflux of molecules such as anticancer drugs to the extracellular matrix of tumor cells. P_gp is a member of the ATP-binding cassette (ABC) transporter family that is implicated in cancer multidrug resistance (MDR). Since MDR is a contributor to...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2019.103156
更新日期：2019-10-01 00:00:00
abstract：:Breaking a carbon-hydrogen bond adjacent to a carbonyl is a slow step in a large number of chemical reactions. However, many enzymes are capable of catalyzing this reaction with great efficiency. One of the most proficient of these enzymes is 3-oxo-Delta5-steroid isomerase (KSI), which catalyzes the isomerization of a...
journal_title：Bioorganic chemistry
pub_type： 杂志文章,评审
doi：10.1016/j.bioorg.2004.06.005
更新日期：2004-10-01 00:00:00
abstract：:Convenient structures such as 2,4-diketo esters have been widely used as an effective pattern in medicinal chemistry and pharmacology for drug discovery. 2,4-Diketonate is a common scaffold that can be found in many biologically active and naturally occurring compounds. Also, many 2,4-diketo ester derivatives have bee...
journal_title：Bioorganic chemistry
pub_type： 杂志文章,评审
doi：10.1016/j.bioorg.2020.104343
更新日期：2020-12-01 00:00:00
abstract：:Inspired with an increasing environmental awareness, we performed an eco-friendly amenable process for the synthesis of silver nanoparticles (AgNPs) using the catkins of Piper longum as an alternative approach with the existing methods of using plant extracts. The fabrication of nanoparticles occurred within 10 min. T...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104230
更新日期：2020-10-01 00:00:00
abstract：:Pulmonary fibrosis is a progressive, irreversible, and fatal fibrotic lung disease with a high mortality and morbidity, and commonly nonresponsive to conventional therapy. Inula japonica Thunb. is a traditional Chinese medicine, known as "Xuan Fu Hua" in Chinese, and has been widely applied to relieve cough and dyspne...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104065
更新日期：2020-09-01 00:00:00
abstract：:A series of bis-indolone-N-oxides, 1a-f, was prepared from bis(ethynyl)benzenes and o-halonitroaryls and studied for their in vitro antiplasmodial activities against Plasmodium falciparum and representative strains of bacteria and candida as well as for their cytotoxicity against a human tumor cell line (MCF7). They d...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2013.03.001
更新日期：2013-06-01 00:00:00
abstract：:Suntamide A (1), a new cyclic peptide, was isolated from Cicadidae Periostracum. The gross structure of 1 was elucidated by detailed analysis of HRMS and 1D/2D NMR spectra, and the absolute configuration was established by C3 Marfey's method. We extended our study to examine biological activity of 1, and found that 1 ...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104493
更新日期：2021-01-01 00:00:00
abstract：:Novel lead compounds as anticancer agents with the ability to circumvent emerging drug resistance have recently gained a great deal of interest. Thiazolidinones are among such compounds with well-established biological activity in the field of oncology. Here, we designed, synthesized and characterized a series of thia...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.104276
更新日期：2020-11-01 00:00:00
abstract：:Xanthatin, a natural sesquiterpene lactone, occurs as one of the major constituents of Xanthium plants (Compositae) and exhibits many important biological properties. To discover natural products-based pesticides, forty-nine Michael-type thiol/amino adducts of xanthatin were synthesized and characterized, while their ...
journal_title：Bioorganic chemistry
pub_type： 杂志文章
doi：10.1016/j.bioorg.2020.103696
更新日期：2020-04-01 00:00:00
