831222-66-3

Upstream product

• 621-59-0 isovanillin 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 97315-18-9 p-methoxy-m-(tert-butyldimethylsilyloxy)-benzaldehyde 
• 86-81-7 3,4,5-trimethoxy-benzaldehyde 
• 39201-89-3 3,4,5-trimethoxybenzaldehyde oxime 
• 831222-65-2 tert-butyl-(2-methoxy-5-vinylphenoxy)dimethylsilane 

Downstream Products

• 1227738-15-9 2-(3-methoxy-4-(3-(2-methoxy-5-(3-(3,4,5-trimethoxyphenyl)-4,5-dihydroisoxazol-5-yl)phenoxy)propoxy)phenyl)-2,3-dihydroquinazolin-4(1H)-one 
• 1227738-16-0 2-(3-methoxy-4-(4-(2-methoxy-5-(3-(3,4,5-trimethoxyphenyl)-4,5-dihydroisoxazol-5-yl)phenoxy)butoxy)phenyl)-2,3-dihydroquinazolin-4(1H)-one 
• 831222-67-4 5-[3-(tert-butyldimethylsilanyloxy)-4-methoxyphenyl]-3-(3,4,5-trimethoxyphenyl)isoxazole 

Relevant academic research and scientific papers

Amidobenzothiazoles And Process For The Preparation Thereof

The present invention provides a compound of general formulae A useful as potential anti-cancer agents against human cancer cell lines and a process for the preparation thereof. Where in R, R1, R2═H, alkyl, alkoxy, halo, haloalkyl, halomethoxy, nitro and G= Where in R, R1, R2═H, alkyl, alkoxy, halo, haloalkyl, halomethoxy, nitro and G=

Synthesis and biological evaluation of 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydroquinazolinone hybrids as anticancer agents

A series of new 3,5-diaryl isoxazoline/isoxazole linked 2,3-dihydro quinazolinone hybrids with different linker architectures have been designed and synthesized. These compounds have been evaluated for their anticancer activity. One of the compounds 4c amongst this series has shown promising anticancer activity. Further some detailed biological assays relating to the cell cycle aspects and tubulin depolymerization activity have been examined with a view to understand the mechanism of action of this conjugate.

Design, synthesis and biological evaluation of 3,5-diaryl-isoxazoline/ isoxazole-pyrrolobenzodiazepine conjugates as potential anticancer agents

A series of 3,5-diaryl-isoxazoline/isoxazole linked pyrrolo[2,1-c][1,4] benzodiazepine (PBD) conjugates were prepared. These conjugates showed potent anticancer activity with GI50 values in the range of 0.1-3.6 μM. Some of these PBD conjugates (6a-c) with promising anticancer activity were further investigated on the cell cycle distribution. Moreover, these PBD conjugates exhibited G0/G1 arrest, enhancement in the levels of p53 protein as well as mitochondrial-mediated intrinsic pathway, leading to release of cytochrome c, activation of caspase-3, cleavage of PARP and subsequent apoptotic cell death. Hence these PBD conjugates with 6a being the most potent one could be be taken up for preclinical studies either alone or in combination with existing therapies. New class of 3,5-diaryl-isoxazoline/isoxazole- pyrrolobenzodiazepine conjugates were prepared and evaluated for their anticancer activity. Further, some of the biological assays related to mechanism aspects were also carried out.

COMBRETASTATIN DERIVATIVES WITH CYTOTOXIC ACTION

The invention described herein relates to new combretastatin derivatives obtained by total synthesis and having the following general formula (I) in which the groups are as defined in the description here below. Said compounds, though chemically related to the structure of cis/trans-combretastatin, do not always bind tubulin, but nevertheless exhibit cytotoxic activity of interest in the oncological field as anticancer and/or antiangiogenic agents.

Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines

Two new series of combretastatin (CA-4) analogues have been prepared. The alkenyl motif of CA-4 was replaced either by a five-membered heterocyclic (isoxazoline or isoxazole) or by a six-membered ring (pyridine or benzene). The new compounds have been evaluated for their effects on tubulin assembly and for cytotoxic and apoptotic activities. Five compounds (18b, 20a, 21a, 34b, and 35b) demonstrated an attractive profile of cytotoxicity (IC50 1 μM) and apoptosis-inducing activity but poor antitubulin activity. The isoxazoline derivatives 18b, 20a, and 21a, demonstrated potent apoptotic activity different from that of natural CA-4. Their ability to block most cells in the G2 phase suggests that these compounds could act on targets different from the mitotic spindle. This would indicate activation of both the intrinsic and the extrinsic apoptotic pathways. The data suggest unambiguously that structural alteration of the stilbene motif of CA-4 can be extremely effective in producing potent apoptosis-inducing agents.