Bicyclic Derivatives of the Potent Dual Aromatase-Steroid Sulfatase Inhibitor 2-Bromo-4-{[(4-cyanophenyl)(4H-1,2,4-triazol-4-yl)amino]methyl}phenylsulfamate: Synthesis, SAR, Crystal Structure, and in vitro and in vivo Activities

Background: Deoxypodophyllotoxin, isolated from theTraditional Chinese Medicine Anthriscus sylvestris, is well-known because of its significant antitumor activity with strong toxicity in vitro and in vivo. Objective: In this article, we synthesized a series of deoxypodophyllotoxin derivatives, and evaluated their antitumor effectiveness.Methods:The anti tumor activity of deoxypodophyllotoxin derivatives was investigated by the MTT method. Apoptosis percentage was measured by flow cytometer analysis using Annexin-V-FITC. Results: The derivatives revealed obvious cytotoxicity in the MTT assay by decreasing the number of late cancer cells. The decrease of Bcl-2/Bax could be observed in MCF-7, HepG2, HT-29 andMG-63 using Annexin V-FITC. The ratio of Bcl-2/Bax in the administration group was decreased, which was determined by the ELISA kit. Conclusion: The derivatives of deoxypodophyllotoxin could induce apoptosis in tumor cell lines by influencing Bcl-2/Bax.

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Synthesis, in vitro and in vivo antitumor activity of symmetrical bis-Schiff base derivatives of isatin

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2013.04.040 ◽

2014 ◽

Vol 74 ◽

pp. 742-750 ◽

Cited By ~ 57

Author(s):

Chengyuan Liang ◽

Juan Xia ◽

Dong Lei ◽

Xiang Li ◽

Qizheng Yao ◽

...

Keyword(s):

Schiff Base ◽

Antitumor Activity ◽

Schiff Base Derivatives ◽

In Vivo Antitumor Activity ◽

Derivatives Of

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Synthesis, in vitro and in vivo activity of benzophenone-based inhibitors of steroid sulfatase

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2004.02.040 ◽

2004 ◽

Vol 12 (10) ◽

pp. 2759-2772 ◽

Cited By ~ 35

Author(s):

Hatem A.M Hejaz ◽

L.W.Lawrence Woo ◽

Atul Purohit ◽

Michael J Reed ◽

Barry V.L Potter

Keyword(s):

Steroid Sulfatase

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Synthesis, characterization and in vitro and in vivo anticancer activity of Pt(iv) derivatives of [Pt(1S,2S-DACH)(5,6-dimethyl-1,10-phenanthroline)]

Dalton Transactions ◽

10.1039/c7dt01054k ◽

2017 ◽

Vol 46 (21) ◽

pp. 7005-7019 ◽

Cited By ~ 25

Author(s):

Benjamin W. J. Harper ◽

Emanuele Petruzzella ◽

Roman Sirota ◽

Fernanda Fabiola Faccioli ◽

Janice R. Aldrich-Wright ◽

...

Keyword(s):

Anticancer Activity ◽

Biological Evaluation ◽

Synthesis And Biological Evaluation ◽

Derivatives Of

Synthesis and biological evaluation in vitro and in vivo of functionalized Pt(iv) derivatives of Pt56MeSS.

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Effects of dietary alteration of bicarbonate and magnesium on rat bone

AJP Renal Physiology ◽

10.1152/ajprenal.1986.250.2.f302 ◽

1986 ◽

Vol 250 (2) ◽

pp. F302-F307 ◽

Cited By ~ 4

Author(s):

J. M. Burnell ◽

C. Liu ◽

A. G. Miller ◽

E. Teubner

Keyword(s):

Crystal Structure ◽

Bone Formation ◽

X Ray Diffraction ◽

X Ray ◽

Growing Rats ◽

Final Composition ◽

Rat Bone

To study the effects of bicarbonate and magnesium on bone, mild acidosis and/or hypermagnesemia were produced in growing rats by feeding ammonium chloride and/or magnesium sulfate. Bone composition, quantitative histomorphometry, and mineral x-ray diffraction (XRD) characteristics were measured after 6 wk of treatment. The results demonstrated that both acidosis (decreased HCO3) and hypermagnesemia inhibited periosteal bone formation, and, when combined, results were summative; and the previously observed in vitro role of HCO3- and Mg2+ as inhibitors of crystal growth were confirmed in vivo. XRD measurements demonstrated that decreased plasma HCO3 resulted in larger crystals and increased Mg resulted in smaller crystals. However, the combined XRD effects of acidosis and hypermagnesemia resembled acidosis alone. It is postulated that the final composition and crystal structure of bone are strongly influenced by HCO3- and Mg2+, and the effects are mediated by the combined influence on both osteoblastic bone formation and the growth of hydroxyapatite.

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Stem-loops direct precise processing of 3′ UTR-derived small RNA MicL

10.1101/341578 ◽

2018 ◽

Author(s):

Taylor B Updegrove ◽

Andrew B Kouse ◽

Katarzyna J Bandyra ◽

Gisela Storz

Keyword(s):

Small Rna ◽

Cleavage Site ◽

Differential Sensitivity ◽

Rnase E ◽

Small Regulatory Rnas ◽

Regulatory Rnas ◽

Derivatives Of

AbstractIncreasing numbers of 3′UTR-derived small, regulatory RNAs (sRNAs) are being discovered in bacteria, most generated by cleavage from longer transcripts. The enzyme required for these cleavages has been reported to be RNase E, the major endoribonuclease in enterica bacteria. Previous studies investigating RNase E have come to a range of different conclusions regarding the determinants for RNase E processing. To understand the sequence and structure determinants for the precise processing of the 3′ UTR-derived sRNAs, we examined the cleavage of multiple mutant and chimeric derivatives of the 3′ UTR-derived MicL sRNA in vivo and in vitro. Our results revealed that tandem stem-loops 3′ to the cleavage site define optimal, correctly-positioned cleavage of MicL and likely other similar sRNAs. Moreover, our assays of MicL, ArcZ and CpxQ showed that sRNAs exhibit differential sensitivity to RNase E, likely a consequence of a hierarchy of sRNA features recognized by the endonuclease.

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