Search for physiologically active compounds

Kumari, Sudesh; Rao, K. S. R. Krishna Mohan; Rao, N. V. Subba

doi:10.1007/bf03047284

Cited by 5 publications

(1 citation statement)

References 8 publications

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“…On the other hand, some flavonoids possessing amino groups are known, but their previously mentioned biological activities are scarcely known. [32][33][34][35] Moreover, to the best of our knowledge, 5-aminoflavones are not known except for only a few examples. 36,37 Therefore, we hypothesized that flavone derivatives substituted with amino groups, which can function as hydrogen bond donors or acceptors as hydroxyl groups, might exhibit antitumor activity in breast cancer.…”

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confidence: 99%

Novel 5-Aminoflavone Derivatives as Specific Antitumor Agents in Breast Cancer

et al. 1996

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In the course of our search for new antitumor agents in breast cancer, novel amino-substituted flavone derivatives were synthesized and examined for antitumor activities. Among them, 5,4'-diaminoflavone and some of its congeners showed remarkable antiproliferative activity against the estrogen receptor (ER)-positive and estrogen-responsive human breast cancer cell line MCF-7. The activity was observed irrespective of the presence or absence of estrogen. The 5-aminoflavone derivatives (5-AFs) are not classical anti-estrogens because they did not compete with [3H]estradiol to bind the estrogen receptor. Moreover, 5-AFs showed antitumor activity highly selective to the ER-positive breast cancer cell line, and they showed no effects against the ER-negative human cancer cell lines HeLa S3, WiDr, and MDA-MB-453. Although the mechanism of their selective antitumor activity to ER-positive breast cancer cells is unclear, 5-AFs are expected to be a new type of antitumor agents in breast cancer.

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confidence: 99%