The minor base convolinine was synthesized. The activity of alkaloids from plants of the genus Convolvulus and their derivatives against HeLa and Hep cancer cell cultures and primary fibroblast culture was studied. It was found that the alkaloid convolvine and its derivatives exhibited cytotoxic activity. The alkaloids N-benzylconvolvine (4) and N-chloroacetylconvolvine (5) at concentrations of 10 Pg/mL exhibited the greatest activity against HeLa and Hep cancer cell cultures. The percent suppression of HeLa cervical carcinoma cells by alkaloid 4 was 35%; of Hep laryngeal cancer cells, 81.6%.A multitude of antitumor drugs are currently produced from alkaloids of plant origin. These include vinblastine, vincristine, and vinorelbine from Vinca rosea L.; docetaxel, from Taxus baccata; etoposide, from Podophyllum peltatum L., etc. The antitumor activity of the alkaloids and their derivatives is due to their influence mainly on cellular metabolism during the M-phase of the cell cycle (mitosis) through binding to tubulin molecules in microtubules. They prevent polymerization of this protein, retard formation of the division spindle (assembly of microtubules), and stop mitosis at the metaphase stage [1].The goal of the present work was to find compounds with cytotoxic activity among alkaloids of the genus Convolvulus (Convolvulaceae) and their derivatives. These alkaloids belong to the tropane class and were isolated from plants of the genus Convolvulus (C. subhirsutus, C. krauseanus, C. pseudocanthabrica) in the Central Asian flora [2].The three alkaloids convolvine (1), convolidine (2), and convolinine (3) were isolated from plants of the genus Convolvulus [3,4]. N-Benzylconvolvine (4) and N-chloroacetylconvolvine (5) are synthetic analogs of convolvine [5].Because convolinine (3) is a minor alkaloid of C. subhirsutus [6], it was synthesized from convolvine in order to study its cytotoxic properties. Its content in C. subhirsutus is 0.25-0.35% of the air-dried raw material mass [3]. The reaction of 1 and ethylenechlorohydrin (6) in the presence of Et 3 N produced 3, which was identical to the natural alkaloid convolinine according to spectral properties (see Experimental).