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Purine and Purine Isostere Derivatives of Ferrocene: An Evaluation of ADME, Antitumor and Electrochemical Properties

Rep, Valentina; Piškor, Martina; Šimek, Helena; Mišetić, Petra; Grbčić, Petra; Padovan, Jasna; Gabelica Marković, Vesna; Jadreško, Dijana; Pavelić, Krešimir; Kraljević Pavelić, Sandra; Raić-Malić, Silvana (2020) Purine and Purine Isostere Derivatives of Ferrocene: An Evaluation of ADME, Antitumor and Electrochemical Properties. Molecules, 25 (7). ISSN 1996-1944

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Abstract

Novel purine and purine isosteres containing a ferrocene motif and 4, 1-disubstituted (11a−11c, 12a−12c, 13a−13c, 14a−14c, 15a−15c, 16a, 23a−23c, 24a−24c, 25a−25c) and 1, 4-disubstituted (34a−34c and 35a−35c) 1, 2, 3-triazole rings were synthesized. The most potent cytotoxic effect on colorectal adenocarcinoma (SW620) was exerted by the 6-chloro-7-deazapurine 11c (IC50 = 9.07 µM), 6-chloropurine 13a (IC50 = 14.38 µM) and 15b (IC50 = 15.50 µM) ferrocenylalkyl derivatives. The N-9 isomer of 6-chloropurine 13a containing ferrocenylmethylene unit showed a favourable in vitro physicochemical and ADME properties including high solubility, moderate permeability and good metabolic stability in human liver microsomes.

Item Type: Article
Uncontrolled Keywords: purine ; ferrocene ; cytostatic activity ; permeability ; microsomal stability
Subjects: NATURAL SCIENCES > Chemistry
Divisions: Division for Marine and Enviromental Research
Projects:
Project titleProject leaderProject codeProject type
Novi spojevi temeljeni na bioizosterima purina za ispitivanje njihovih antitumorskih i antipatogenih djelovanjaRaić-Malić, SilvanaIP-2018-01-4682HRZZ
Depositing User: Dijana Jadreško
Date Deposited: 07 Jan 2021 12:47
Last Modified: 07 Jan 2021 12:47
URI: http://fulir.irb.hr/id/eprint/6154
DOI: 10.3390/molecules25071570

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