scholarly journals Tandem MS-Based Metabolite Profiling of 19,20-Epoxycytochalasin C Reveals the Importance of a Hydroxy Group at the C7 Position for Biological Activity

ACS Omega ◽  
2021 ◽  
Vol 6 (5) ◽  
pp. 3717-3726
Author(s):  
Manoj Kushwaha ◽  
Arem Qayum ◽  
Shreyans K. Jain ◽  
Jasvinder Singh ◽  
Amit Kumar Srivastava ◽  
...  
Keyword(s):  
Biological Activity ◽  
Hydroxy Group ◽  
Metabolite Profiling ◽  
Tandem Ms

Synthesis and Biological Activity of New 16,17-Secoestrone Derivatives

2000 ◽  
Vol 65 (1) ◽  
pp. 77-82 ◽  
Author(s):  
Suzana Jovanović-Šanta ◽  
Silvana Andrić ◽  
Radmila Kovačević ◽  
Vjera Pejanović
Keyword(s):  
Biological Activity ◽  
Hydroxy Group ◽  
Sodium Borohydride ◽  
Estrogenic Activity ◽  
Complete Loss ◽  
Borohydride Reduction ◽  
Experimental Animals ◽  
Biological Tests ◽  
Sodium Borohydride Reduction

Starting from estrone 3-benzyloxy-17β-hydroxyestra-1,3,5(10)-trien-16-one oxime (3b) was synthesized, which underwent Beckmann fragmentation giving the 3-benzyloxy-17-oxo- 16,17-secoestra-1,3,5(10)-triene-16-nitrile (4b). Sodium borohydride reduction of this compound afforded 3-benzyloxy-17-hydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile (5b). The deprotection of the 3-hydroxy group was achieved by action of hydrogen upon derivatives 4b and 5b in presence of Pd/C as a catalyst, yielding 3-hydroxy-17-oxo-16,17-secoestra- 1,3,5(10)-triene-16-nitrile (4a) and 3,17-dihydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile (5a). In biological tests on experimental animals, compounds 4a, 4b, 5a and 5b showed virtually a complete loss of estrogenic activity, whereas compounds 4a, 5a and 5b exhibited moderate antiestrogenic effect.

The synthesis of 5-methyl-19-nor-5β-pregna-9,16-diene-3,20-dione, 5-methyl-19-nor-5β-pregna-9,10-diene-3,6,20-trione and their analogues with annellated E ring

1991 ◽  
Vol 56 (12) ◽  
pp. 2892-2905 ◽  
Author(s):  
Jiří Polman ◽  
Alexander Kasal
Keyword(s):  
Biological Activity ◽  
Hydroxy Group ◽  
Skeletal Rearrangements ◽  
Key Steps

The synthesis of compounds VII, XVII, XXXIV and XXXVII is described, in which biological activity is assumed. The key steps of their preparation are the dehalogenation of compound XVIII and radicalic deoxygenation of the 6β-hydroxy group in compound XXX, which take place without skeletal rearrangements.

Moulting Hormones. LIII. the Synthesis and Biological Activity of Some Ecdysone Analogues

1981 ◽  
Vol 34 (12) ◽  
pp. 2607 ◽  
Author(s):  
M Galbraith ◽  
DS Horn ◽  
B Kelly ◽  
J Kinnear ◽  
M Martin ◽  
...  
Keyword(s):  
Biological Activity ◽  
Hydroxy Group ◽  
Structural Changes ◽  
Mosquito Larvae ◽  
Moulting Hormones

A number of ecdysone analogues were prepared to study the effect of structural changes on biological activity. It was found that analogues with the 5α-configuration or a 3,5-cyclo structure were inactive, that a 3β-hydroxy group enhances activity but is not essential for activity, and that 3β-substituents decrease activity as follows: OMe (60%), OAc (25%) and OEt (10%). The keto diol (3), keto alcohol (9) and amide (36) were found to be highly toxic to mosquito larvae.

Synthesis and Biological Activity of Phencyclidine Homologues with para-Hydroxy-Group in the Aromatic Ring.

ChemInform ◽  
2005 ◽  
Vol 36 (34) ◽  
Author(s):  
V. A. Glushkov ◽  
L. V. Anikina ◽  
Yu. B. Vikharev ◽  
O. G. Stryapunina ◽  
Yu. V. Shklyaev ◽  
...  
Keyword(s):  
Biological Activity ◽  
Aromatic Ring ◽  
Hydroxy Group

Virus-Like Particles in a Human Breast Cancer: Structural Similarity to Previously Reported Particles

1973 ◽  
Vol 31 ◽  
pp. 378-379
Author(s):  
G. Kasnic ◽  
S. E. Stewart ◽  
C. Urbanski
Keyword(s):  
Breast Cancer ◽  
Biological Activity ◽  
Human Breast Cancer ◽  
Osteogenic Sarcoma ◽  
Human Tumor ◽  
Structural Similarity ◽  
Cell Tumor ◽  
Human Breast ◽  
Human Tumor Cell ◽  
Type Particle

We have reported the maturation of an intracisternal A-type particle in murine plasma cell tumor cultures and three human tumor cell cultures (rhabdomyosarcoma, lung adenocarcinoma, and osteogenic sarcoma) after IUDR-DMSO activation. In all of these studies the A-type particle seems to develop into a form with an electron dense nucleoid, presumably mature, which is also intracisternal. A similar intracisternal A-type particle has been described in leukemic guinea pigs. Although no biological activity has yet been demonstrated for these particles, on morphologic grounds, and by the manner in which they develop within the cell, they may represent members of the same family of viruses.

Effects of Vincristine on Endothelial Microtubules in the Spinal Cord

1976 ◽  
Vol 34 ◽  
pp. 58-59
Author(s):  
John L. Beggs ◽  
John D. Waggener ◽  
Wanda Miller
Keyword(s):  
Spinal Cord ◽  
Biological Activity ◽  
Horseradish Peroxidase ◽  
Transport Mechanism ◽  
Vasogenic Edema ◽  
Vesicular Transport ◽  
Close Proximity

Microtubules (MT) are versatile organelles participating in a wide variety of biological activity. MT involvement in the movement and transport of cytoplasmic components has been well documented. In the course of our study on trauma-induced vasogenic edema in the spinal cord we have concluded that endothelial vesicles contribute to the edema process. Using horseradish peroxidase as a vascular tracer, labeled endothelial vesicles were present in all situations expected if a vesicular transport mechanism was in operation. Frequently,labeled vesicles coalesced to form channels that appeared to traverse the endothelium. The presence of MT in close proximity to labeled vesicles sugg ested that MT may play a role in vesicular activity.

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