Synthesis and cytotoxic studies of a new series quinolinoxymethylcoumarins

4-Bromomethylcoumarins (1a-k) were reacted with 8-hydroxyquinolines (2a-b) to yield quinolinoxymethylcoumarins (3a-o). The structure of all the synthesized compounds were confirmed by spectral studies and screened for their anticancer activities against Dalton's Ascitic Lymphoma (DAL) and Ehrlich Ascites Carcinoma (EAC) cell lines. Out of these, the compound (3d) (R = 6-Benzyl, R1=H) was found to be the most potent cytotoxic compound against DAL cell line with IC50 value of 45.86 μg/mL and the compound (3i) (R = 6-i-Pr, R1= CH3) against EAC cell line with IC50 value of 39.26 μg/mL

Synthesis and antimicrobial studies on novel sulfonamides containing 4-azidomethyl coumarin

A series of new and novel coumarin-6-sulfonamides with a free C4-azidomethyl group have been synthesized as antimicrobials in three steps starting from 7-methyl-4-bromomethylcoumarin 1. The reaction of 1 with chlorosulfonic acid was found to yield the corresponding 6-sulfonylchloride 2, which when treated with sodium azide led to intermediate 3. The title sulfonamides 5a-y were obtained from the reaction of 3 with various aromatic amines 4 in refluxing benzene. The chemical structures of the compounds were elucidated by IR, NMR and LC-MS spectral data. All the synthesized compounds have been screened for their in vitro anti-bacterial and anti-fungal activities. Some of the compounds have been found to be active against both bacterial species at a concentration of 1 μg/mL. © 2009 Elsevier Masson SAS. All rights reserved

Microwave assisted synthesis of dihydrobenzo4,5imidazo1,2-apyrimidin-4- ones; Synthesis, in vitro antimicrobial and anticancer activities of novel coumarin substituted dihydrobenzo4,5imidazo1,2-apyrimidin-4-ones

The present article describes the synthesis of dihydrobenzo4,5imidazo1, 2-apyrimidin-4-one (2a-h) under microwave irradiation. The product was obtained in excellent yield (74-94%) in a shorter reaction time (2 min). These molecules (2a, b) further reacted with various substituted 4-bromomethylcoumarins (3a-f) to yield a new series of coumarin substituted dihydrobenzo4,5imidazo1,2-a pyrimidin-4-ones (4a-h). The structure of all the synthesized compounds were confirmed by spectral studies and screened for their in vitro antibacterial activity against three Gram-positive bacteria viz., Staphylococcus aureus, Enterococcus faecalis, Streptococcus mutans and three Gram-negative bacteria viz., Escherichia coli, Klebsiella pneumonia, Pseudomonas aeruginosa and antifungal activity against Candida albicans, Aspergillus niger, Aspergillus fumigatus, Aspergillus flavus, Fusarium oxysporum, Penicilliumchrysogenum and anticancer activity against Dalton's Ascitic Lymphoma (DAL) cell line. In general, all the compounds possessed better antifungal properties than antibacterial properties. The coumarin substituted dihydrobenzo4,5imidazo1,2- apyrimidin-4-one (4g) (R = i-Pr, R1 = 6-Cl) was found to be the most potent cytotoxic compound (88%) against Dalton's Ascitic Lymphoma cell line at the concentration of 100 μg/mL. © 2013 Elsevier Masson SAS. All rights reserved