7or-(4'-Amino)phenylthio-l,4-androstadiene-3,17-dione(7a-APTADD), a potent enzyme-activated irreversible inhibitor, was examined in two different human cell culture lines, MCF-7 human mammary carcinoma cells and JAr choriocarcinoma cells. Both the MCF-7 and JAr cell culture systems exhibit aromatase activity, and 7a-APTADD was evaluated for its aromatase-inhibitory activity, for its ability to ...

in view of potential biological activities of small molecule polyamides, we synthesized some novel n-(2-aminoethyl)-1-benzyl-2- (alkylthio)-1h-imidazole-5-carboxamide (7a,b), and n-(2-(1-benzyl-2-(alkylthio) -1h-imidazole- 5-carboxamido) ethyl)-1-benzyl-2- (alkylthio)-1h-imidazole-5-carboxamides (8a,b) as antitumor agents. the antitumor activity of compounds 7a,b and 8a,b was studied at concent...

7or-(4'-Amino)phenylthio-l,4-androstadiene-3,17-dione(7a-APTADD), a potent enzyme-activated irreversible inhibitor, was examined in two different human cell culture lines, MCF-7 human mammary carcinoma cells and JAr choriocarcinoma cells. Both the MCF-7 and JAr cell culture systems exhibit aromatase activity, and 7a-APTADD was evaluated for its aromatase-inhibitory activity, for its ability to ...

The synthesis of novel amide derivatives of benzosuberone 7a-j from commercially available benzosuberone was successfully achieved in six steps. Some of the important reactions that are involved in the synthesis are (i) insertion of methylester (ii) Suzki reaction and (iii) saponification followed by amide bond formation. The newly synthesis benzosuberone derivatives 7a-j were screened for anti...

In the title compound, C(26)H(31)NO(3), the octa-hydro-1H-isoindole ring is not planar and the two rings are twisted with a C-C-C-C torsion angle of 73.6 (4)°. The six-membered ring has a chair conformation while the five-membered ring has an envelope conformation on the C-atom in position 7a. The H atoms in the 3a- and 7a-psitions are cis and the H-C-C-H torsion angle is 42.36°.

2-Amino-5-nitro-6-ribitylamino-4(3H)-pyrimidinone (7) was phosphorylated with chlorophosphoric acid yielding an isomer mixture containing about 63% of the 5'-phosphate 7a together with other monophosphates and bisphosphates of 7. Preparative HPLC afforded pure 7a. Catalytic hydrogenation of 7a yields the labile substrate of pyrimidine deaminase, 2,5-diamino-6-ribitylamino-4(3H)-pyrimidinone 5'-...

This study involved a campaign to isolate and study additional latrunculin analogues from two taxonomically unrelated sponges, Cacospongia mycofijiensis and Negombata magnifica. A total of 13 latrunculin analogues were obtained by four different ways, reisolation (1-4), our repository (5, 6), new derivatives (7-12), and a synthetic analogue (7a). The structures of the new metabolites were eluci...

Influenza A virus poses serious health threat to humans. Neutralizing antibodies against the highly conserved M2 ion channel is thought to offer broad protection against influenza A viruses. Here, we screened synthetic Camel single-domain antibody (VHH) libraries against native M2 ion channel protein. One of the isolated VHHs, M2-7A, specifically bound to M2-expressed cell membrane as well as i...

Four polymerizable α-phosphonooxy phosphonic acids 7a, 7b, 9 and 16 were synthesized in seven steps. They were characterized by 1H, 13C and 31P NMR spectroscopy and by high-resolution mass spectroscopy. The copolymerization of acidic monomers 7a, 7b, 9 and 16 with 2-hydroxyethyl methacrylate was studied using a differential scanning calorimeter. Due to the presence of two acidic groups, those m...