376357-56-1

Upstream product

• 13291-18-4 isopropenylmagnesium bromide 
• 106731-74-2 tert-butyl[(2S)-oxiran-2-ylmethoxy]diphenylsilane 
• 58479-61-1 tert-butylchlorodiphenylsilane 
• 107033-46-5 (R)-(tert-butyldiphenylsilyloxy)methyloxirane 

Downstream Products

• 397868-70-1 C₂₅H₃₄O₂Si 
• 1552276-13-7 C₃₀H₃₆O₃Si 
• 1552276-20-6 C₁₄H₁₆O₃ 
• 1552276-07-9 (S)-5-(tert-Butyldiphenylsilyloxy)-4-hydroxypentan-2-one 
• 1552276-09-1 (2S,4S)-1-(tert-butyldiphenylsilyloxy)-4-methylhex-5-ene-2,4-diol 
• 1552276-11-5 (2S,4R)-1-(tert-butyldiphenylsilyloxy)-4-methylhex-5-ene-2,4-diol 
• 1552276-15-9 ((2R,4S,6S)-6-methyl-2-phenyl-6-vinyl-1,3-dioxan-4-yl)methanol 
• 1518769-82-8 C₂₄H₂₈O₃Si 
• 1518769-89-5 C₂₃H₂₈O₃Si 

Relevant academic research and scientific papers

Enantioselective synthesis of spliceostatin e and evaluation of biological activity

An enantioselective total synthesis of spliceostatin E has been accomplished. The δ-lactone unit A was constructed from readily available (R)-glycidyl alcohol using a ring-closing olefin metathesis as the key reaction. A cross-metathesis of ring A containing δ-lactone and the functionalized tetrahydropyran B-ring provided spliceostatin E. Our biological evaluation of synthetic spliceostatin E revealed that it does not inhibit splicing in vitro and does not impact speckle morphology in cells. Spliceostatin E was reported to possess potent antitumor activity.

Antimalarial diterpenoid dimers of a new carbon skeleton from Aphanamixis grandifolia

Chemical investigation into the minor constituents of Aphanamixis grandifolia yielded three new diterpenoid dimers, aphadilactones E-G (1-3) featuring a new carbon skeleton. Their structures and absolute configurations were fully established by comprehensive spectroscopic data analysis and ECD calculation. Discovery of another two new dimers (4 and 5) suggested the structure of recently reported aphanamene A to be re-investigated. Compounds 1-5 showed moderate antimalarial activities with low micromolar IC50 values.

Aphadilactones a-d, four diterpenoid dimers with dgat inhibitory and antimalarial activities from a meliaceae plant

Aphadilactones A-D (1-4), four diastereoisomers possessing an unprecedented carbon skeleton, were isolated from the Meliaceae plant Aphanamixis grandifolia. Their challenging structures and absolute configurations were determined by a combination of spectroscopic data, chemical degradation, fragment synthesis, experimental CD spectra, and ECD calculations. Aphadilactone C (3) with the 5S,11S,5'S,11'S configuration showed potent and selective inhibition against the diacylglycerol O-acyltransferase-1 (DGAT- 1) enzyme (IC50 = 0.46 ± 0.09 μM, selectivity index > 217) and is the strongest natural DGAT-1 inhibitor discovered to date. In addition, compounds 1-4 showed significant antimalarial activities with IC50 values of 190 ± 60, 1350 ± 150, 170 ± 10, and 120 ± 50 nM, respectively.

Synthetic studies on polymaxenolides: Model studies for constructing dihydropyran portion and synthesis of lower portion

With a goal of the total synthesis of polymaxenolide, the first hybrid marine natural product, the model studies for constructing the dihydropyran portion based on the originally proposed biosynthesis (C-C bond formation followed by dehydrative cyclization) and the synthesis of the lower portion (the C1-C3, C7-C17 portion) based on an iodide-induced Morita-Baylis-Hillman type reaction (a three-component assembly) followed by Suzuki-Miyaura cross-coupling are described.

LAULIMALIDE ANALOGS AND USES THEREOF

The present invention provides compounds having formula 1: (I) and pharmaceutically acceptable derivatives thereof, wherein R1-R10, q, t, X0, X1, A, B, D, E, G, J, K, L, M and Z are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders associated with cellular hyperproliferation.