Synthesis of active organic molecules to be drug

The family Labiatae (= Lamiaceae) is a rich family, which is located in the temperate climate zone, naturally grown in Mediterranean countries and cultured in many countries. This family contains about 200 genera and over 3000 species. Oleanolic acid (OA) is a naturally occurring pentacyclic triterpenoid found indifferent family plants which exhibits various biological activities, including antimicrobial, anti-inflammatory, anti-diabetic and cytotoxic activities. Twelve different (12) oleanan structures were identified in the in-silico tests. Among the determined species, compound 3β,11α-dihydroxy-1,12-diene oleanolic acid showed the best binding affinity to the homology model of the c-Rel/c-Rel / IκBα enzyme. The synthesis of the target molecule 1β,2α,3β,11α-tetrahydroxy-oleanane-12-ene,3-acetyl was performed in two steps starting whit the oleanolic acid. In the first step, the β-amyrin was obtained and in the second step, starting whit the synthesized β-amyrin or 3β-hydroxy-oleanane-12-ene-28-oic acid methyl ester, the target molecule synthesis studies were performed. In the synthesis steps, 25 triterpenes having different stereoisomers were synthesized. The nine (9) triterpenes having structure of the oleanan were synthesized for the first time in the literature. β-amyrin is a triterpene with a very high commercial cost and in our study β-amyrin's synthesis was completed in three steps with a very high yield of 66% in total. All synthesized compounds were evaluated for cytotoxic activity on standard healthy fibroblast 3T3 cell lines derived from Swiss albino mouse embryo tissue. The effects of triterpenes were determined by ATP cell viability values. First, the cytotoxicity of cells containing different triterpenes was determined as the dose-response relationship. 3T3 cells (15 x 103 cells total in each well) were exposed to various concentrations of triterpenes (1.56-200 μM) for 24 hours. The synthesized triterpenes showed proliferative activity at low concentrations (1.56 μM) and showed increased toxicity at increasing concentrations. A series of oleanolic acid analogues showed anti-proliferative activity at higher concentrations (6.25 to 200 μM) and the highest activity was observed whith erythrodiol. Keywords: Labiatae (=Lamiaceae), Oleanolic acid, Oleanane, β-Amylin, Erythrodiol, Doking, Ctotoxitic, Proliferative / Anti-proliferative, Triterpenes