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Novel Thiophenes, Thienopyrimidines, and Triazolothienopyrimidines for the Evaluation of Anticancer and Augmentation Effects of γ‐Radiation
Author(s) -
Shaaban Mohamed A.,
Ghorab Mostafa M.,
Heiba Helmy I.,
Kamel Mona M.,
Zaher Nashwa H.,
Mostafa Mohamed I.
Publication year - 2010
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200900150
Subject(s) - doxorubicin , in vitro , chemistry , stereochemistry , cytotoxic t cell , combinatorial chemistry , pharmacology , biochemistry , chemotherapy , biology , genetics
New derivatives of thiophenes 2 , 12 , iminoaminothieno[2,3‐ d ]pyrimidines 3 , 5 , and 6 , triazolothieno[2,3‐ d ]pyrimidines 8–11 , pyrazolo‐ and triazinothieno[2,3‐ d ]pyrimidines 4 , 7 , respectively, have been prepared by different synthetic procedures. Structure elucidation of the newly synthesized compounds was carried out via elemental analyses and spectral data. The antitumor activity of compounds 2 , 3 , and 9–12 was evaluated against in‐vitro cell lines (HEPG‐2 and MCF‐7). Compounds 2 , 3 , 10 , 11 , and 12 showed significant in‐vitro cytotoxic activity against hepatocellular carcinoma (HEPG‐2) compared to the reference drug Doxorubicin. Compound 2 showed significant in‐vitro cytotoxic activity against breast cancer (MCF‐7) cells compared to the reference drug Doxorubicin. The augmenting effect of γ‐radiation was assessed; here, compounds 2 , 3 , 10 , and 11 showed the most potent in‐vitro anticancer activity.