Syntheses and antitumor activities of N′1, N′3-dialkyl-N′1,N′3-di- (alkylcarbonothioyl) malonohydrazide: The discovery of elesclomol
A series of N′1,N′3-dialkyl- N′1,N′3-di(alkylcarbonothioyl) malonohydrazides have been designed and synthesized as anticancer agents by targeting oxidative stress and Hsp70 induction. Structure-activity relationship (SAR) studies lead to the discovery of STA-4783 (elesclomol), a novel small molecule that has been evaluated in a number of clinical trials as an anticancer agent in combination with Taxol.
Silver ion-mediated desulfurization of N,N-disubstituted 2-hydroxythiobenzamides
Silver ion-mediated desulfurization of N-(2-hydroxythiobenzoyl)morpholine (1a) or -piperidine (1b) was used to develop a new synthetic method for heterocycles such as 1,3-benzoxazin-1-ium salts. 2-Amino-4-morpholino- and 2-amino-4-piperidino-1,3-benzoxazi
Examinations of thioamides and their derivatives. X. Salts 1-(o-hydroxy)-alpha-alkylthiobenzylidene) piperidinium, structure, properties and biological activity
In reactions of 1-(o-hydroxy)thiobenzoylpiperidine with alkyl halides there was obtained 1-(o-hydroxy-alpha-alkylthiobenzylidene)piperidinium bromides and iodides. Structure of obtained compounds have been determined by spectroscopic methods. Products of hydrolysis their and antimitotic and enzymatic activity were investigated too.
Santus,Soltysiak,Smolinski,Stefaniak
p. 189 - 193
(2007/10/02)
Infrared spectra of several thiopiperidides and thiomorpholides
Infrared spectra in the 1700-500 cm-1 region have been studied for several types of thiopiperidides (thiobenzoylpiperidides, thiocinnamoylpiperidides and phenylthioacetpiperidides) and for the corresponding thiomorpholides.Three characteristic thioamide bands were located and assigned.The behaviour of these bands on molecular complexing (with iodine as an electron acceptor) was used to support the assignments.The experimental data were discussed in terms of the theoretical results obtained by an HMO procedure.