1380328-07-3

Upstream product

• 1380328-06-2 C₁₆H₃₄OS₂Si 
• 1380328-05-1 (R)-2-((2R,3R)-7-(3-(benzyloxy)phenyl)-3-((4-methoxybenzyl)oxy)heptan-2-yl)oxirane 
• 1380328-04-0 C₂₄H₃₀O₅ 
• 1380328-03-9 (3S,4R)-8-(3-(benzyloxy)phenyl)-3-methyloct-1-en-4-ol 
• 289034-17-9 C₁₈H₂₀O₂ 

Downstream Products

• 1380328-08-4 (R)-7-(2-(((2R,4S,5R,6R)-6-(4-(3-(benzyloxy)phenyl)butyl)-2-(4-methoxyphenyl)-5-methyl-1,3-dioxan-4-yl)methyl)-1,3-dithian-2-yl)-7-methyloct-1-en-4-ol 
• 1380328-10-8 C₅₁H₆₄O₈ 
• 1380328-11-9 C₄₈H₆₈O₉Si 
• 1380327-88-7 (1R,3R,4R,5S,9R,13R)-9-(hydroxymethyl)-3-(4-(3-hydroxyphenyl)butyl)-4,16,16-trimethyl-2,6,10,17-tetraoxatricyclo[11.3.1.1^1,5]octadecane-7,11-dione 

Relevant academic research and scientific papers

New [apurishiatokishin[apurishiatokishin] derivative containing anticancer agents

The invention provides an aplysiatoxin derivative represented by formula (I), or a pharmaceutically acceptable salt thereof, that is a PKC activator having no carcinogenesis-promoting activity that can serve as an alternative to Bryo-1 as a novel compound that can be used as an anticancer agent. (In formula (I), R1 is a hydrogen atom or hydroxyl group; R2 is a hydrogen atom or methyl group; R3 is a hydrogen atom or methyl group; R4 is a hydrogen atom or methyl group; R5 is a hydrogen atom or methyl group; and R6 is represented by a substituent selected from any of a hydrogen atom, halogen atom, acetylamino group, hydroxyl group, or optionally substituted alkyl group having 1-5 carbon atoms.)

Structure-activity studies on the spiroketal moiety of a simplified analogue of debromoaplysiatoxin with antiproliferative activity

Aplog-1, a simplified analogue of tumor-promoting debromoaplysiatoxin, is antiproliferative but not tumor-promoting. Our recent study has suggested that local hydrophobicity around the spiroketal moiety is a crucial determinant for antiproliferative activity. To further clarify the structural features relevant to the activity, we synthesized two methyl derivatives of aplog-1, where a methyl group was installed at position 4 or 10 of the spiroketal moiety. 10-Methyl-aplog-1 (5) bound to the C1B domains of novel PKCs (δ, η, and θ) with subnanomolar Ki values, approximately 10-20 times stronger than aplog-1, and markedly inhibited the growth of many human cancer cell lines, while 4-methyl-aplog-1 (4) had levels of activity similar to those of aplog-1. Interestingly, 5 showed little tumor-promoting activity unlike the tumor promoter debromoaplysiatoxin. These results suggest that 5 is a potent PKC ligand without tumor-promoting activity and could be a therapeutic lead for the treatment of cancer, like bryostatins.