NDLI: Synthesis, anticancer, anti-HIV-1, and antimicrobial activity of some tricyclic triazino and triazolo[4,3-e]purine derivatives

Content Provider	Springer Nature Link
Author	Ashour, Fawzia A. Rida, Samia M. El Hawash, Soad A. M. ElSemary, Mona M. Badr, Mona H.
Copyright Year	2011
Abstract	In an effort to etablish new candidates with improved antineoplastic, anti-HIV-1 and antimicrobial activities, the synthesis of some new triazino and triazolo[4,3-e]purine derivatives is described: 6,8-dimethyl-1,4-dihydro-1,2,4-triazino[4,3-e]purine-7,9(6H, 8H)-diones 3–6; 5,7,9-trimethyl-1,2,4-triazolo[4,3-e]purine-6,8(5H, 7H, 9H)-diones 11–13, together with the synthesis of the 8-substituted purine derivative: 8-(3,5-diamino-1H-pyrazol-4-yl)diazenyl-1,3-dimethyl-1H-purine-2,6(3H, 7H)-dione 7. The prepared compounds were tested for their in vitro anticancer, anti-HIV and antimicrobial activities. The results of the in vitro anticancer screening revealed that compound 3 exhibited considerable activity against melanoma MALME-3 M, non-small lung cancer HOP-92 and breast cancer T-47D (GI50 values of 25.2, 31.8, and 32.9 μM, respectively). The anti-HIV-1 results indicated that compounds 7 and 13c displayed moderate activity (maximum % cell protection 30.52 and 35.54 at 2 × 10−4 M, respectively). The in vitro antimicrobial data showed that compound 12 was the most active against P. aeruginosa, it was equipotent to ampicillin (MIC < 100 μg/ml). While compound 11d was the most active against P. vulgaris, it was as active as ampicillin (MIC < 50 μg/ml). In addition, compounds 12 and 13c were the most active against S. aureus (MIC <50 and <25 μg/ml, respectively). On the other hand, the tested compounds devoid of antifungal activity except 6b and 11c which showed weak activity against A. niger.
Starting Page	1107
Ending Page	1119
Page Count	13
File Format	PDF
ISSN	10542523
Journal	Medicinal Chemistry Research
Volume Number	21
Issue Number	7
e-ISSN	15548120
Language	English
Publisher	Springer-Verlag
Publisher Date	2011-03-27
Publisher Place	New York
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Purines Anticancer Anti-HIV Antimicrobial activity Biochemistry Cell Biology Pharmacology/Toxicology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology, Toxicology and Pharmaceutics

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