Synthesis and biological evaluation of novel 1,5-benzothiazepin-4 (5h)-ones as potent antiangiogenic and antioxidant agents

Deepu, C. V. and Raghavendra, G. M. and Rekha, N. D. and Mantelingu, K. and Rangappa, K. S. and Bhadregowda, D. G. (2015) Synthesis and biological evaluation of novel 1,5-benzothiazepin-4 (5h)-ones as potent antiangiogenic and antioxidant agents. Current Chemistry Letters, 4 (4). pp. 133-144.

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Abstract

Novel 1,5-benzothiazepin-4-(5H)-one derivatives (8a-8g) have been synthesized by intramolecular cyclization of 6 using propyl phosphonic anhydride (T3P) as a cyclodehydrating agent. The anti-angiogenic and anti-oxidant properties of the new derivatives were then evaluated. Compounds 8b, 8d, 8e, 8f and 8g exhibited very good inhibition of capillary proliferation, thus proving their anti-angiogenic properties. In addition, the in vitro antioxidant activities of these compounds were evaluated using diphenyl picryl hydrazine (DPPH), OH-, metal ion-chelating and NO (nitric oxide) assays, and the results compared with butylated hydroxytoluene (BHT), a well known anti-oxidant. Compounds 8a-8g showed excellent free-radical scavenging activities in the metal ion-chelating assay, and compounds 8f and 8g showed nitric oxide radical scavenging properties at a concentration of 20-100 µg/mL, and are thus more potent than BHT.

Item Type:	Article
Uncontrolled Keywords:	1-5-Benzothiazepin-4 (5H)-Ones and Anti-Angiogenic and Anti-Oxidants and T3P
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry Yuvaraj college > Chemistry
Depositing User:	Users 19 not found.
Date Deposited:	25 Jul 2019 06:35
Last Modified:	25 Jul 2019 06:35
URI:	http://eprints.uni-mysore.ac.in/id/eprint/5549

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