New retinoid derivatives as back-ups of Adarotene.

@article{Giannini2012NewRD,
  title={New retinoid derivatives as back-ups of Adarotene.},
  author={Giuseppe Giannini and Tiziana Brunetti and Gianfranco Battistuzzi and Domenico Alloatti and Gianandrea Quattrociocchi and Maria Grazia Cima and Lucio Merlini and Sabrina Dallavalle and Raffaella Cincinelli and Raffaella Nannei and Loredana Vesci and Federica Bucci and Rosanna Foder{\`a} and Mario Berardino Guglielmi and Claudio Pisano and Walter Cabri},
  journal={Bioorganic \& medicinal chemistry},
  year={2012},
  volume={20 7},
  pages={
          2405-15
        }
}
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References

SHOWING 1-10 OF 28 REFERENCES
A novel atypical retinoid endowed with proapoptotic and antitumor activity.
TLDR
Following oral administration, 4 was well tolerated and caused tumor growth inhibition in the ovarian carcinoma, A2780/DX, and in the human melanoma, MeWo, growing in nude mice, thus supporting the therapeutic interest of the novel agent.
Cellular and Pharmacological Bases of the Antitumor Activity of a Novel Adamantyl Retinoid, ST1926
TLDR
The more marked antitumor effect showed by ST1926 in immuno-competent mice rather than in tumor xenografts suggests a contribution of indirect host-mediated antitumors effects in addition to a direct antiproliferative activity against tumor cells.
Synthesis and structure-activity relationships of a new series of retinoid-related biphenyl-4-ylacrylic acids endowed with antiproliferative and proapoptotic activity.
TLDR
It appears that the presence of the carboxylic group is an essential requirement for apoptogenic properties but not for antiproliferative activity, this being maintained in amide derivatives.
Cyclization-activated prodrugs. Basic carbamates of 4-hydroxyanisole.
TLDR
A detailed study of the N-methyl-N-[2-(methylamino)ethyl]carbamate showed that generation of the parent phenol followed first-order kinetics with t1/2 = 36.3 min at pH 7.4, 37 degrees C, and was accompanied by formation of N,N'-dimethylimidazolidinone.
Drug Metabolism for the Perplexed Medicinal Chemist
  • B. Testa
  • Biology
    Chemistry & biodiversity
  • 2009
TLDR
The toxicological consequences of metabolism at the molecular, macromolecular, and macroscopic levels are manyfold and a brief overview is offered together with a summary of the reactions of toxification and detoxification of the antiepileptic valproic acid.
A prodrug approach to increasing the oral potency of a phenolic drug. 1. Synthesis, characterization, and stability of an O-(imidomethyl) derivative of 17 beta-estradiol.
TLDR
The results suggest that an O-(imidomethyl) type prodrug is insensitive to enzymatic catalysis of hydrolysis yet may hydrolyze quickly enough to release 17 beta-estradiol faster than 17 Beta-ESTradiol is conjugated and excreted.
Tumor targeting by covalent conjugation of a natural fatty acid to paclitaxel.
TLDR
Tumor targeting of the conjugate was demonstrated by pharmacokinetic studies in M109 tumor-bearing mice, indicating an area under the drug concentration-time curve of DHA-paclitaxel in tumors that is 8-fold higher than pac litaxel at equimolar doses and 57-foldHigher at equitoxic doses.
Retinoid related molecules an emerging class of apoptotic agents with promising therapeutic potential in oncology: pharmacological activity and mechanisms of action.
TLDR
A critical overview of the current knowledge on the pharmacology of RRMs is presented, focussing on such issues as the spectrum of cytotoxic activity, the molecular mechanisms of action and the pre-clinical basis of clinical development.
ST1926, a novel and orally active retinoid-related molecule inducing apoptosis in myeloid leukemia cells: modulation of intracellular calcium homeostasis.
TLDR
A novel chemical series designed against the RRM prototype, CD437, including molecules with apoptotic effects in acute promyelocytic leukemia and other myelogenous leukemia cell lines, as well as ST2065, an RRM with antagonistic properties.
Qualitative structure-metabolism relationships in the hydrolysis of carbamates
The aims of this review were 1) to compile a large number of reliable literature data on the metabolic hydrolysis of medicinal carbamates and 2) to extract from such data a qualitative relation
...
1
2
3
...