Search

The optimization and structure–activity relationship of 4,5-dihydropyrrolo[3,4-c]pyrazol-6(1H)-ones were performed in this manuscript. Most of the compounds showed higher PPI inhibitory activities and antiproliferative activities.

Ten new water-soluble amino acid derivatives of pyropheophorbide-aethers 4a–4jwere designed and synthesized via3 steps reaction using pyropheophorbide-aas key intermediate. All target compounds exhibited better phototoxicity than BPD-MA and the most phototoxic compound 4dand 4jindividually showed IC50values of 41nmol/L and 33nmol/L against HCT116 cell, which represented 7.8- and 9.7-fold increase of antitumor potency compared to BPD-MA.

Isomers of evodiamine derivatives 2and 3were obtained by straightforward asymmetric total synthesis and their antitumor activity was investigated. All the four isomers exhibited good to excellent antitumor potency.

A series of novel E-ring modified evodiamine derivatives were designed and synthesized as antitumor agents. Compound 12showed good antitumor activity with a broad spectrum, which acted by dual inhibition of topoisomerase I and II.

The structure–activity relationship of a tetrahydrocarbazole antifungal lead compound was investigated. Several targeted compounds showed potent activity against Candidaspecies. Particularly, the most active compound 13ican be used as a good starting point for the discovery of novel antifungal agents.

The pyrolysis of biomass is a promising way for production of bio-gasoline if the stability and quality problems of the bio-crude-oil can be solved by catalytic cracking and reforming. In this paper, an on-line infrared spectrum was used to study the characteristics of catalytic pyrolysis with the following preliminary results. The removal of CO of organic acid is more difficult than that of aldehydes and ketones. HUSY/γ-Al2O3 and REY/γ-Al2O3 catalysts exhibited better deoxygenating activities while HZSM-5/γ-Al2O3 catalyst exhibited preferred selectivities for production of iso-alkanes and aromatics. Finally, possible mechanisms of biomass catalytic pyrolysis are discussed as well.

Both enantiomers of amphetamine hydrochloride were stereospecifically synthesised based on bakers’ yeast reduction of phenylacetone. A simple and efficient method for the chiral inversion of (S)-1-phenyl-2-propanol 3to (R)-1-phenyl-2-propanol 8has been discussed.

The SN2 reaction of enantiopure sulfonate‐protected alcohols, e.g. (I) and (IV), with carboxylic acids (II) and (V) in the presence of tertiary amines (Et3N or DBU) proceeds with inversion of the stereocenter to give acyl‐protected alcohols, e.g. (III) and (VI), in good yields and high to excellent stereoselectivity.