[New antitumor derivatives of vinblastine].
The alkaloids of Catharanthus roseus vincristine 1 and vinblastine 2 are widely used in the chemotherapy of cancer. Their nitro-derivatives have also antitumour activity [2]. The dinitro-derivatives 4, 6-9 were prepared for pharmacological investigation. Some new hydroxymethyl derivatives 12-14, 17-18, 23-24 of the antitumour indole-indoline alkaloids vinblastine 2 and leurosine 5 were synthetised in two different ways a) by the selective reduction of 2, 5 or deacetoxy-vinblastine 16, b) by the ferric chloride mediated coupling reaction of catharanthine 19 and the corresponding vindoline derivatives 21, 22. Synthetising 24 a new bisvindoline 25 was the main product. 13 and 14 showed cytotoxic activity for small cell lung cancer LXFS 650.
Bölcskei
H
H
Richter Gedeon Vegyészeti Gyár Rt., Budapest.
Szántay
C
C
Mák
M
M
Balázs
M
M
Szántay
C
C
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D018288:Carcinoma, Small Cell / Q000188:drug therapy; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy; D051379:Mice; D008819:Mice, Nude; D015394:Molecular Structure; D014183:Transplantation, Heterologous; D014747:Vinblastine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D014748:Vinca Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use
D000970:Antineoplastic Agents; D014748:Vinca Alkaloids; D014747:Vinblastine
Uj, antitumor hatású vinblasztin származékok.