T1 - Synthesis and biological activity of analogs of fecapentaene-12

Aeberli P, Gogerty JH, Houlihan WJ, Iorio LC. Synthesis and central nervous system depressant activity of some bicyclic amides. J Med Chem 1976;19(3):436-8.

T1 - Synthesis and biological activity of mycalolide analogs

T1 - Synthesis and biological activity of a biotinylated vasopressin analog

T1 - Synthesis and biological activity of sarcodictyins

(Formyl-sarcosine) 1-LH-RH (I), (acetyl-sarcosine) 1-LH-RH (II), (2-pyrrolidone-4-carboxylic acid) 1-LH-RH (III), (N-methyl-2-pyrrolidone-4-carboxylic acid) 1-LH-RH (IV), hydroxyproline 1-LH-RH (V) and (cyclopentane-carboxylic acid) 1-LH-RH (VI) were synthesized by solid phase methods on a benzhydrylamine resin support. Peptides I-IV were assayed for LH- and FSH-releasing activity over a 4-h period after subcutaneous injection into immature male rats in order to detect any prolongation of activity. The peptides were found to have the following integrated LH-releasing activities compared with LH-RH: I, 64%; II, 72%; III, 19%; IV, 58%. None of the peptides were found to be longer acting than LH-RH. Peptides V and VI were far less active, 0.001% and 1.4%, respectively.

SUCCINIMIDES: SYNTHESIS, REACTION AND BIOLOGICAL ACTIVITY

N2 - (Formyl-sarcosine) 1-LH-RH (I), (acetyl-sarcosine) 1-LH-RH (II), (2-pyrrolidone-4-carboxylic acid) 1-LH-RH (III), (N-methyl-2-pyrrolidone-4-carboxylic acid) 1-LH-RH (IV), hydroxyproline 1-LH-RH (V) and (cyclopentane-carboxylic acid) 1-LH-RH (VI) were synthesized by solid phase methods on a benzhydrylamine resin support. Peptides I-IV were assayed for LH- and FSH-releasing activity over a 4-h period after subcutaneous injection into immature male rats in order to detect any prolongation of activity. The peptides were found to have the following integrated LH-releasing activities compared with LH-RH: I, 64%; II, 72%; III, 19%; IV, 58%. None of the peptides were found to be longer acting than LH-RH. Peptides V and VI were far less active, 0.001% and 1.4%, respectively.


Synthesis and biological activity of some new benzophenothiazines

AB - GEMZAR® (gemcitabine·HCl) is a difluorinated analog of deoxy cytidine. It was initially synthesized as a novel anti-viral compound with broad spectrum in vitro activity against both RNA and DNA viruses. However, the compound proved to have a narrow therapeutic index when it was administered daily during the in vivo evaluation of antiviral activity. Using a staggered schedule of administration, GEMZAR is found to be a potent antitumor agent in murine and human xenograft solid tumor models. Studies have shown that gemcitabine diphosphate is a ribonucleotide reductase inhibitor, whereas the triphosphate is a potent and unique terminator of DNA synthesis. In phase I studies a variety of dose schedules were investigated. Based on phase I studies including pharmacokinetic data, phase II studies were initiated. Activity was observed in a variety of solid tumors. The results are specially encouraging for non-small cell lung and pancreatic cancer. GEMZAR is currently undergoing registration review of the Phase III clinical trials for treatment of non-small cell lung and pancreatic cancer.

Diketopiperazines: Biological Activity and Synthesis

AB - Mycalolide analog 4, consisting only of the side chain of mycalolide B (2), a trisoxazole macrolide of marine origin, was stereoselectively synthesized using Roush crotylboration, an Evans aldol reaction, and a Paterson aldol reaction as key steps. The analog 4 was found to have strong actin-depolymerizing activity.

Synthesis and biological activity of nitrogen …

Flavanones have been a potential source in the search for lead compounds and biologically active components and have been the focus of much researches and development in the last 30 years.

Synthesis and the Biological Activity of ..

N2 - Mycalolide analog 4, consisting only of the side chain of mycalolide B (2), a trisoxazole macrolide of marine origin, was stereoselectively synthesized using Roush crotylboration, an Evans aldol reaction, and a Paterson aldol reaction as key steps. The analog 4 was found to have strong actin-depolymerizing activity.