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Synthesis and anti-proliferative activity evaluation of sorafenib derivatives with a 3-arylacryloyl hydrazide unit
Springer Science and Business Media LLC - Tập 24 - Trang 1733-1743 - 2014
A series of sorafenib derivatives with a 3-arylacryloyl hydrazide unit were designed and synthesized, and their anti-proliferative activity against human cancer cell lines (ACHN, HCT116, MDA-MB-231) were evaluated by MTT assay. Most of the synthesized compounds showed superior or similar cytotoxicity against the selected cell lines to the control sorafenib. Among these derivatives, compounds 8a, 8...... hiện toàn bộ
A novel chromonyl thiohydantoin with anti-proliferative action on primary hepatocellular carcinoma cells
Springer Science and Business Media LLC - Tập 27 - Trang 153-160 - 2017
Chromone, imidazolidinedione, thiohydantoin and 2,4-thiazolidinedione structures are known to be cytotoxic to cancer cells. In this study, biological activities of previously synthesized 18 chromonyl-2,4-thiazolidinediones/imidazolidinediones/thiohydantoins were tested by sulforhodamine B assay in five liver and one breast cancer cell lines. It was shown that a hybrid chromonyl thiohydantoin deriv...... hiện toàn bộ
Design, synthesis, and biological evaluation of quinazoline derivatives as α-glucosidase inhibitors
Springer Science and Business Media LLC - Tập 24 - Trang 2227-2237 - 2014
To develop a lead anti-diabetic compound, a series of 21 novel quinazoline derivatives have been synthesized and screened against α-glucosidase. The binding mode of the compounds at the active site of α-glucosidase was explored using Glide docking method. The binding model suggests one to four hydrogen bonding interactions between quinazoline derivatives and α-glucosidase. 6-Bromo-2-cyclopropyl qu...... hiện toàn bộ
Design, synthesis, anticancer evaluation and molecular docking studies of new imidazo [2, 1-b] thiazole -based chalcones
Springer Science and Business Media LLC - Tập 31 - Trang 1369-1383 - 2022
A new series of imidazo[2, 1-b]thiazole-based chalcone derivatives were designed, synthesized, and tested for their anticancer activities. Firstly, the cytotoxic ability of the compounds was tested on three different types of cancer cells, namely colorectal adenocarcinoma (HT-29), lung carcinoma (A-549), breast adenocarcinoma (MCF-7), and mouse fibroblast cells (3T3-L1) by XTT tests. Afterwards, f...... hiện toàn bộ
Study of solvent effects on structural and conformational properties of cimetidine tautomers
Springer Science and Business Media LLC - Tập 25 - Trang 2042-2057 - 2016
One of the members of a class of medications is cimetidine that is called H2-receptor antagonist or H2 blockers. Cimetidine reduced the amount of acid secreted by the lining cells of the stomach. It is commonly used in treatment of gastro-esophageal reflux disease and peptic ulcer disease. In this study, the cimetidine’s tautomers stability, structural data, HOMO, LUMO orbitals (energies and shape...... hiện toàn bộ
Diversifying the xanthine scaffold for potential phosphodiesterase 9A inhibitors: synthesis and validation
Springer Science and Business Media LLC - Tập 30 - Trang 1199-1219 - 2021
Xanthine and its derivatives have been a great area of interest for the development of potent bioactive agents. In this study, two synthesis routes have been developed for 1,3,8-tri substituted xanthine derivatives. The synthesis routes exploits “xanthine” as precursor molecule as it represents maximum unsubstituted sites for maximum possible substitutions. This study divulged the reactivity patte...... hiện toàn bộ
Antidiabetic activity and histopathological analysis of carnosol isolated from Artemisia indica linn in streptozotocin-induced diabetic rats
Springer Science and Business Media LLC - Tập 26 - Trang 335-343 - 2016
Diabetes mellitus is a major metabolic disorder affecting a huge population all over the world. The aim of the current study was to validate the folkloric use of Artemisia indica as an antidiabetic plant by using the isolated compound carnosol from the chloroform fraction of Artemisia indica in streptozotocin-induced diabetes mellitus in rats. The antidiabetic activity-guided isolation of the chlo...... hiện toàn bộ
Synthesis, structure-activity relationship studies and evaluation of a TLR 3/8/9 agonist and its analogues
Springer Science and Business Media LLC - Tập 30 - Trang 1377-1385 - 2021
A comprehensive SAR study of a putative TLR 3/8/9 agonist was conducted. Despite the excitement surrounding the potential of the first small molecule TLR3 agonist with a compound that additionally displayed agonist activity for TLR8 and TLR9, compound 1 displayed disappointing activity in our hands, failing to match the potency (EC50) reported and displaying only a low efficacy for the extent of s...... hiện toàn bộ
Microwave-induced CAN promoted atom-economic synthesis of 1H-benzo[b]xanthene and 4H-benzo[g]chromene derivatives of N-allyl quinolone and their antimicrobial activity
Springer Science and Business Media LLC - Tập 22 - Trang 2954-2963 - 2012
Some new 1H-benzo[b]xanthene and 4H-benzo[g]chromene derivatives of N-allyl quinolone were efficiently synthesized via microwave-induced one-pot three component reaction of N-allyl quinolones, 2-hydroxy-1,4-naphthoquinone and cyclic β-diketones/malononitrile, and iso-propylcyanoacetate in the presence of catalytic amount of ceric ammonium nitrate under solvent-free condition. This methodology allo...... hiện toàn bộ
Effect of the lipophilic parameter (log P) on the anti-parasitic activity of imidazo[1,2-a]pyridine derivatives
Springer Science and Business Media LLC - Tập 21 Số 4 - Trang 415-420 - 2012
A number of imidazo[1,2-a]pyridine derivatives were selected and investigated in relation to anti-parasitic (Trichomonas vaginalis) activity. After treatment with derivatives, biological activity was assessed by determination of the in vitro viability of cell cultures, using alamar blue as a metabolic indicator. A good correlation was found between the anti-parasitic activity and the partition coe...... hiện toàn bộ
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