The one-pot synthesis of three dragmacidin derivatives is reported. Sarcosine anhydride (4) is brominated and immediately reacted with the corresponding indole to produce the products, namely 3,6-bis(5'-methoxy-3'-indolyl)-1,4-dimethylpiperazine-2,5-dione (1), 3,6-bis(7'-methyl-3'-indolyl)-1,4-dimethylpiperazine-2,5-dione (2) and 3,6-bis-(6'-chloro-3'-indolyl)-1,4-dimethylpiperazine-2,5-dione (...

Three new abietane-type diterpenoids, 7a-butoxyabieta-8,12-diene-11,14-dione (1), 6a,7a-dihydroxyabieta-8,12-dien-11,14-dione (2), and 6a,7b-dihydroxyabieta8,12-diene-11,14-dione (3) were isolated from the bark of Cryptomeria japonica D. Don. Their structures were established by means of 1D and 2D NMR, IR, UV, and HR-EI-MS spectra and comparison with the data of known analogues. ã 2016 Publishe...

In order to know the contribution of adrenal and gonadal androgens to the development of the side gland of Suncus murinus, we studied the effects of gonadectomy and adrenalectomy on gland thickness and the plasma levels of testosterone, androstenedione (delta 4-dione) and dehydroepiandrosterone (DHA). In males, castration decreased gland thickness to 71% of the control. The plasma levels of del...

A simple synthetic strategy to C 2-symmetric bis-spiro-pyrano cage compound 7 involving ring-closing metathesis is reported. The hexacyclic dione 10 was prepared from simple and readily available starting materials such as 1,4-naphthoquinone and cyclopentadiene. The synthesis of an unprecedented octacyclic cage compound through intramolecular Diels-Alder (DA) reaction as a key step is described...

Several steroids occurring in the pathway of corticosteroid biosynthesis were investigated for their ability to exert a fast or delayed feedback inhibition of stress-induced release of corticotrophin. Rats were injected subcutaneously with vehicle or a steroid either 10 min (fast feedback) or 4 h (delayed feedback) before they were subjected to stress which consisted of a 2 min exposure to ethe...

This paper describes the properties and partial purification from Pseudomonas testosteroni of enzymes concerned with the introduction of unsaturation into ring A of 3-ketosteroids. These enzymes promote the formation of the A1e4-diene-3-one structure from steroids bearing C-19 angular methyl groups and the formation of ring A phenols from lQ-nor-steroids. P. testosteroni is a strict aerobe whic...

Five new podocarpane-type trinorditerpenes were isolated from the bark of Taiwania cryptomerioides. Structures of 1beta, 14-dihydroxy-13-methoxy-6,8,11,13-podocarpatetraene (1), 1beta, 14-dihydroxy-13-methoxy-8,11,13-podocarpatriene (2), 13-hydroxy-12-methoxy-8,11,13-podocarpatrien-3-one (3), 14-hydroxy-13-methoxy-1,8,11,13-podocarpatetraen-3-one (4), and 13-methoxy-8,12-podocarpatriene-11,14-d...

The hindered diene 1 reacts with 3-methylcyclohexenone 6 catalyzed by triflimide to produce the Mukaiyama Michael product 7 (low-temperature quenching) or the [4+2] cycloadduct 8 (quenching at 0 degrees C). Reaction of the hindered diene 23 with 2-methylcyclohexenone 12 with 5:1 AlBr3:AlMe3 afforded a 71% yield of a 1.9:1 mixture of two cycloadducts. Hydrolysis of the major isomer gave the dion...

mycobacterium smegmatis ptcc 1307 (cip 73.26) was used as a microbial agent to produce androsta-1,4-diene-3,17-dione (add) and androst-4-ene-3,17-dione, two useful precursors in the synthesis of steroid drugs. the side chain of cholesterol, as the substrate, was selectively cleaved in the presence of five enzyme inhibitors. an intermediate structure with intact side chain, cholest-4-ene-3-one, ...

Insulin-like growth factor-1 receptor (IGF-1R) is a growth factor receptor tyrosine kinase acting as a critical mediator of cell proliferation and survival. Novel 5-benzylidenethiazolidine-2,4-dione (5) and 5-(furan-2-ylmethylene)thiazolidine-2,4-dione (6) compounds were identified as potent and selective IGF-1R inhibitors via hierarchical virtual screening. Initial SAR and biological activity ...