Про все позиции мне понятна их "антилекарственность", так как известен механизм, кроме тиомочевин. А чем собственно тиомочевины не угодили? Многие тиомочевины проявляют цитотоксический эффект. Их аж 11 тыс штук в pubmede протестированно.Submission of structures containing problematic linkages or functional groups for successful drug development (e.g. nitro, nitroso, -N-N-, -N=N-, imine, semicarbazone,thioamides, thioureas) are discouraged.
Вот нашел:
Есть ли, у уважаемых коллег, какие либо соображения по поводу беспереспективности тиомочевин ?http://www.inchem.org/documents/cicads/ ... .htm#8.6.2
Thiourea at concentrations of 30–300 mmol/litre induced single strand breaks in the DNA of primary cultures of isolated rat hepatocytes (Sina et al., 1983). The inhibitory effect of thiourea on the induction of DNA strand breakage due to various intercalating substances in mouse leukaemia cells might be the result of a change in chromatin structure. This could alter the activity of a topoisomerase responsible for the occurrence of strand breaks in cooperation with the intercalating substances (Pommier et al., 1983). The methods of detection of UDS were either autoradiography or liquid scintillation counting, and the DNA single strand breaks were detected with the alkaline elution assay.
