Synthesis of some potential antiestrogenic agents

Some novel steroidal arylidene derivatives were synthesized and representative examples were tested for their antiestrogenic activity. The active compounds were subjected for antitumor activity screening. The compounds tested displayed aromatase inhibitory activity as shown by decrease in estradiol and increase in testosterone levels. Further, some compounds were tested for androgenic/anabolic activity. The steroids used for preparation of these arylidene derivatives are the clinically applied: levo-Norgestrel, Testosterone, Mesterolone and Norethisterone

Synthesis and antitumour activity of some acridonamil derivatives

Three series of N-methyl-, N-phenyl and N-benzylacridonanil derivatives have been synthesized [2a-i - 4a-i]. The P388-antileukemic activity has been enaluated

Synthesis, antitumour and antimicrobial activities of 3-chloro-9- [p-N-substituted sulphamoylphenyl-aminomethylene] acridines

The synthesis of a new series of 3-chloro-9-[p-N-substituted sulfamoylphenyl-aminomethylene] acridines is described. The synthesized derivatives were screened for antitumour activity by the in vivo P 388 test and cytotoxic activity by in vitro test against Ehrlich ascites carcinoma. Also, antimicrobial activity of the prepared derivatives was carried out by agar diffusion and MIC methods

Synthesis, antitumour and antimicrobial activities of some new acridine derivatives

A series of 3-chloro-9-[p-N-substituted sulphamoylphenylaminomethyl] acridines has been synthesized. The products have been screened for their antitumour activity against P388 lymphocytic leukemia. Only 3- chloro-9-[p-amidinosulphamoyl phenylaminomethyl] acridine showed presumptive activity. The prepared compounds were also tested for their antimicrobial activity. Most of the compounds exhibited significant antimicrobial activity

Synthesis of 4-methylergosta1,4, 7,22-tetraen-3-one and some other derivatives of ergosterone and cholest-7-en-3one

Selective 4-monomethylation of [Ia] and [Ib] by standard methods was investigated. 4a-methyl-5a-ergosta-7,22-dien-3-one [IIIa] and its 5a-cholest-7-en-3-one analogue were synthesized in a one-step process from [Ia] and [Ib], respectively. Synthesis of the tetraen-3-one [IV] was attempted by different methods, and was obtained through bromination-dehydro-bromination of [IIIa]. Trials for 4-alkoxycarbonylation of [Ia] are also reported