• Journal of Physiology & Pathology in Korean Medicine
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• v.19 no.2
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• pp.441-445
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• 2005

Tripterygium regelii has been used as an oriental medicine, especially antiparasitic, anti-inflammatory and detoxifying agents in East asia. During our research to develop new antitumor agents from natural products, MeOH ext. and CH2Cl2 ext. of Tripterygium regelii showed the potent antitumor activity. In order to purify active compounds from Tripterygium regelii, activity-guided fractionation was carried out. Silica gel and RP-18 column chromatography for the active fraction led to the isolation of two compounds and their antitumor activities were studied. Those two compounds didn't show potent antitumor activity against human tumor cell lines. The structure of two compounds were determined by $^1H-NMR$, $^{13}C-NMR$, DEPT, $^1H-^{13}C$ COSY and IR spectrum. Compound I and Compound II were turned out to be Celastrol, and ${\beta}-sitosteryl-3-o-{\beta}-D-glucopyranoside$ respectively.

• Archives of Pharmacal Research
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• v.20 no.6
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• pp.610-619
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• 1997

Some new 9H-thioxanthen-9-one incorporated into heterocyclic systems such as pyridone 8, pyrazoline 9, pyranone 11, iminopyrane 12, furopyrimidine 17, imidazothiazole 19, thiazole 21, triazine 24 and other related compounds through a para imminophenyl grouping at position-1 of the thioxanthenone ring were synthesized and tested as antitumor agents against L1210 leukemia in mice. Some of the new compounds showed considerable antitumor activity.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.185-185
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• 1998

As part of our continuing attempts to evaluate biologically active compounds from fruiting bodies of cultivated fungus of Paecilomyces japonicus Yasuda, we conducted series of experiments on various fractions and compounds isolated by systematic fractionations. Our main efforts were concentrated on searching for compounds showing antitumor activities, which were tested on mice carrying Sarcoma-180 ascitic tumor. The antitumor activity was assessed by the life spans after these mice were administered Lp. with test compounds for consecutive 20 days. One of two pure compounds, which we have isolated to date, demonstrated significant prolongation of life span. ( Mean Survival Time: 30.3 days compared to that of control: 23.6 days). Structural analysis showed that this compound corresponds to D-mannitol. On the other hand, Ergosterol, another isolated pure compound didn't show efficient antitumor activity. We also obtained water-soluble fractions containing protein-bound polysaccharides and n-butantol fractions, which showed strong antitumor activities, 35.4(150%) and 32.1(136.0%) days of MST, respectively. In SRB assay, however, the test materials didn't show any toxic effects, but the level of acid phosphatase increased significantly when they were applied in cultured macrophage in vitro. Therefore, we concluded that antitumour activities might be attributed to immunostimulating rather than cytotoxic effects. Further experiments are underway to purify and structurally characterize new antitumour compounds from the active fractions.

• Biomolecules & Therapeutics
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• v.9 no.3
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• pp.143-155
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• 2001

Many attention has been focused on developing new chemotherapeutic agents for a treatment of cancer from natural products. From Carpesium divaricatum S. et Z. (Compositae), various monoterpenoid compounds were isolated and exhibited mild antitumor activity against human tumor cell lines. These facts prompted us to explore the structure-activity relationship of these compounds. The synthesis of monoterpenoid compound was accomplished by Fries rearrangement, Grignard reaction, elimination, allylic oxidation, esterification and epoxidation as key steps. The results of in vitro cytotoxicity (A549, SK-OV-3, SK-MEL-2, XF498, HCT15) of the synthesised compounds are as follows: First of all, epoxide moiety is prerequisite for cytotoxic activity in diester compound. Any kind of compounds with olefin or diol moiety instead of epoxide ring exhibited poor or mild cytotoxic activity respectively. Of o-acetoxy and isobutoxy epoxy esters, p-sub-stituted phenylacetate compounds exhibited high cytotoxic activities against SK-MEL-2 and HCT15.

• Archives of Pharmacal Research
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• v.28 no.1
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• pp.39-43
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• 2005

Eight compounds were isolated from the methanolic extract of the twigs of Celtis sinensis through repeated silica gel and Sephadex LH-20 column chromatography. Their chemical structures were elucidated as two triterpenoids, germanicol and epifriedelanol, two amide compounds, trans-N-caffeoyltyramine and cis-N-coumaroyltyramine, two lignan glycoside, pinoresinol glycoside and pinoresinol rutinoside, and two steroids by spectroscopic analysis.

• Bulletin of the Korean Chemical Society
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• v.35 no.5
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• pp.1337-1342
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• 2014

A novel and convenient route for the synthesis of a series of thalidomide derivatives is described. Compound 2 was cyclized with different amines under alkaline condition to obtain 4-nitro substituted phthalimidines 3a-d. Hydroxylactams 4a-d were produced via bromination and hydroxylation. Different acyl chlorides were reacted with hydroxylactams to provide the desired esters 5a-d. All compounds were evaluated by MTT assay for their inhibitory activities against HCT-116, MG-63, MCF-7, HUVEC and HMVEC cell lines in vitro. Most of them showed no obvious cytotoxic effect on normal human cells, compounds 4a-d, $5a_2$, $5a_4$, $5a_5$, $5b_2$, $5c_2$ and $5d_2$ exhibited potent antitumor activities, among which compounds $5a_2$ and $5b_2$ were more effective than 5-FU.

• Archives of Pharmacal Research
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• v.20 no.2
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• pp.138-143
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• 1997

5-Aryl-2,3-dihydroimidazo[2,1-a]isoquinolines were reported to have strong antitumor activity and one of the derivatives such as $5-[4^{l}$ -(piperidinomethyl)phenyl]-2,3-dihydroimidazo[2,1-a] isoquinoline (1, SDZ 62-434) was found to be more effective than the clinical cytostatic agent edelfosine (2) in in vitro and in vivo assays. Currently SDZ 62-434 is in clinical trials in Europe. The structure-activity relationship studies of SDZ 62-434 showed that compounds with substitution on ring A were less active than the lead compound. Ring B in SDZ 62-434 was essential for the activity because compounds without B ring had no antitumor activity. Among the 3-arylisoquinolin-1-one derivatives, $3-[4^{I}$-(piperidinomethyl)phenyl] substituted analog had no antitumor activity but simple phenyl substituted compound, such as 4, showed the most potent antitumor activity in various human tumor cell lines.

• Journal of Microbiology and Biotechnology
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• v.19 no.10
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• pp.1135-1138
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• 2009

The bioassay-guided fractionation of MeOH extract from Naematoloma fasciculare afforded a petroleum ether fraction (NFPF) and four known compounds, which showed good antitumor activities to inhibit MCF-7 cell line proliferation in vitro and tumor growth in $H_{22}$ implanted mice in vivo. In addition, a number of unsaturated aliphatic acids were identified in NFPF by GC analysis. These results showed that NFPF inhibits tumor growth through the activity of unsaturated aliphatic acids together with two active compounds, ergosterol peroxide (1: 62.17 mg/g in NFPF) and ergosterol (2: 3.13 mg/g in NFPF), and indicate the potential utility of NFPF as an antitumor drug.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1998.11a
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• pp.159-160
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• 1998

Results of chemistry and biological activity of many years indicate that plants belonging to the Isodon genus are rich in ent-kaurane diterpenoids, which have been revealed to possess biological activities such as antitumor, antibacterial and antiinflammatory effects. In continuation of our research on diterpenoids in medicinal plants of this genus, the acetone extract from the leaves of I. xerophilus, which is a plant native to Yunnan province of China, showed potent antitumor activity against K562. After partition, the most active EtOAc part was studied. Four new diterpenoids named xerophilusin A(l), B(2), C(3), D(4), and eight known compounds including macrocalin B(5) and rabdorosthomin A(6) were isolated, whose structures were elucidated through a series of one- and two-dimensional NMR techniques(DEPT, COSY, HMQC, HMBC and ROESY experiments). Among them, compound 1, 2 and 5 had two unique epoxy units formed by two ether bridges from C-20 to C-7, C-14. Up to now, there are four compounds having such an peculiar structure besides these three compounds. Compound 3 and 4 were two of the few examples possessing $1{\beta}$ substitutes. All the diterpenoid compounds were subjected to the antitumor screening. It is interesting that only xerophilusin A(l), B(2) and macrocalin(5) exhibited significant antitumor activity against K562 by the method of MTT($IC_{50}$ were listed in Table 1.). The results inspired us to infer that the unique ether bridges from C-20 to C-7, C-14 possibly played an important role in the antitumor activity.

• Archives of Pharmacal Research
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• v.19 no.1
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• pp.62-65
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• 1996

A homologous series of twenty, hitherto unreported, analogues of 5-halosubstituted $1, 3-Bis(\omega-cyanoalkyl)uracil$acyclic nucleosides were synthesized by the series of alkylation reactions of 5-halouracils with the corresponding chloroacetonitrile, chloropropionitrile, chlorobutyronitrile and 5-chlorovaleronitrile $(Cl-(C_ 2)_n-CN: n=l, 2, 3, 4)\; in\; anhydrous\; DMSO\; (or DMF)/K_2CO_3(or NaH)\; under\; 75^{\circ}C$ temperature. Antitumor activities for the synthesized compounds were determined against three cell lines (FM-3A cell, P-388 cell and U-938 cell lines). The compounds that exhibited moderate activity to significant activity, included la-b, 2a-b, 3a-c, and 4a, whose compounds were active against P-388, FM-3A and U-937 cell lines with the compounds la, lb, and 2a, showing significant antitumor activity (inhibitory concentrations $(IC_{50})$ ranged from 2.2 to $7.0\mug/ml$). Their strucrure-activity relationship did not show any activity differences in their effective chain length (methyl, ethyl, propyl, butyl) in 1, 3-bis(.omega.-cyanoalkyl) uracils.