Following the interaction of 2-chloro-N-(5-aryl-1,3,4-oxadiazole-2-yl) acetamides 1a-b with ammonium thiocyanate in dry acetone, the 5-unsubstituted 2-imino-4-thiazolidinones 4a-b have been synthesized. Compounds 4a-b were subsequently utilized in Knoevenagel condensation with aromatic aldehydes or isatin derivatives to synthesize the series of 5-arylidene/isatinylidene substituted 2-(1,3,4-oxadiazol-2-yl)imino-4-thiazolidinones 5a-h and 6a-d. The structures of target compounds were confirmed by using 1H NMR spectroscopy and elemental analysis. Evaluation of anti-cancer activity in
vitro for the synthesized compounds was performed following the National Cancer Institute protocol against leukemia, melanoma, lung, colon, CNS, ovarian, renal, prostate, and breast cancer cell lines. As a result, the most active compound 5a, namely 2-[5-(4-chlorophenyl)-[1,3,4]oxadiazol-2-ylimino]-5-(4-methoxybenzylidene)thiazolidin-4-one was found to be a highly efficient anti-tumor candidate with average logGI50 and logTGI values of -5.19 and -4.09, respectively
UDC: 618.19-009.7-085
More than 82 % of women of reproductive age note pain in the mammary gland. Every fifth woman feels severe pain (mastalgia) and swelling (mastodynia) in the mammary gland. Cyclic mastalgia is combined with hyperprolactinemia. Hyperprolactinemia occurs when dopamine does not suppress pituitary function enough to reduce prolactin release. Agni casti fructus, known for its dopaminergic activity, relieves pain and discomfort in the mammary glands. 50 patients were under observation. Only 10 % of patients felt mild pain, 32 % experienced moderate pain, 50 % assessed it as severe, and 8 % experienced extreme pain. After the treatment, the complete absence of pain was noted by 76 % of patients. The results of the conducted studies indicate a high efficiency of 76 % and the safety of using Agni casti fructus in treating mastalgia and mastodynia. The high efficiency in the treatment of mastalgia and mastodynia with the herbal medicine Agni casti fructus without the additional use of hormonal drugs can be explained by the fact that this drug normalizes the hormonal balance of a woman